Pub Date : 2024-07-12DOI: 10.2174/0115701794317332240610073030
Hong-Ru Dong
: Some new (S)-2-[1-aryl-5-methyl-1H-1,2,3-triazol-4-yl]-4-benzyl-4,5-dihydro-oxa-zoline were synthesized by the reaction of (S)-N-(1-hydroxy-3-phenylpropan-2-yl)-1-aryl-5-me-thyl-1H-1,2,3-triazole-4-carboxamides which were prepared from aromatic amine as starting materials, with p-toluenesulfonyl chloride, triethylamine and DMAP. The structures were char-acterized by 1H NMR, 13C NMR, MS and IR. The synthesized chiral triazole-oxazoline was used as a ligand in the Diels-Alder asymmetric catalytic reaction between 3-allyl-1,3-oxazolidin-2-ketone and 2-methyl-1,3-butadiene, using PdCl2 as catalyst. (S)-3-(4-methylcyclohexe-3-ene-1-formyl)-1,3-oxazolidin-2-one was obtained. Background: The chiral triazole-oxazoline ligands are rarely reported. Objective: The aim of the study was to synthsize some new chiral triazole-oxazoline ligands (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydrooxazoline (5a-g). Methods: The one-pot methods of oriented synthesis were adopted. This study provides a simple and effective method for the synthesis of new chiral triazole-oxazoline derivatives. Results: The some new chiral the triazole-oxazoline ligands (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydrooxazoline (5a-g) were synthesized and the asymmetric Diels-Alder cyclization of 3-allyl-1,3-oxazolidin-2-ketone and 2-methyl-1,3-butadiene was catalyzed by PdCl2 using the synthesized (S)-4-triazole-oxazoline ligands. Conclusion: Some new (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydro-oxazoline was synthesized by corresponding N-[(S)-1-hydroxy-3-phenylpropan-2-yl]-1-aryl-5-methyl-1H-1,2,3-triazole-4-formamide, through one-pot oriented synthesis method. After pre-liminary evaluation, the chiral triazoline-oxazoline ligands, in which 1,2,3-triazole rings, like pyridine-type rings, chiral materials were saved and replace one oxazoline ring in the dioxazoline ligands for asymmetric catalytic reactions.
{"title":"Synthesis of Some New Chiral Triazole-Oxazoline Derivatives","authors":"Hong-Ru Dong","doi":"10.2174/0115701794317332240610073030","DOIUrl":"https://doi.org/10.2174/0115701794317332240610073030","url":null,"abstract":": Some new (S)-2-[1-aryl-5-methyl-1H-1,2,3-triazol-4-yl]-4-benzyl-4,5-dihydro-oxa-zoline were synthesized by the reaction of (S)-N-(1-hydroxy-3-phenylpropan-2-yl)-1-aryl-5-me-thyl-1H-1,2,3-triazole-4-carboxamides which were prepared from aromatic amine as starting materials, with p-toluenesulfonyl chloride, triethylamine and DMAP. The structures were char-acterized by 1H NMR, 13C NMR, MS and IR. The synthesized chiral triazole-oxazoline was used as a ligand in the Diels-Alder asymmetric catalytic reaction between 3-allyl-1,3-oxazolidin-2-ketone and 2-methyl-1,3-butadiene, using PdCl2 as catalyst. (S)-3-(4-methylcyclohexe-3-ene-1-formyl)-1,3-oxazolidin-2-one was obtained. Background: The chiral triazole-oxazoline ligands are rarely reported. Objective: The aim of the study was to synthsize some new chiral triazole-oxazoline ligands (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydrooxazoline (5a-g). Methods: The one-pot methods of oriented synthesis were adopted. This study provides a simple and effective method for the synthesis of new chiral triazole-oxazoline derivatives. Results: The some new chiral the triazole-oxazoline ligands (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydrooxazoline (5a-g) were synthesized and the asymmetric Diels-Alder cyclization of 3-allyl-1,3-oxazolidin-2-ketone and 2-methyl-1,3-butadiene was catalyzed by PdCl2 using the synthesized (S)-4-triazole-oxazoline ligands. Conclusion: Some new (S)-4-benzyl-2-(5-methyl-1-aryl-1H-1,2,3-triazole-4-yl)-4,5-dihydro-oxazoline was synthesized by corresponding N-[(S)-1-hydroxy-3-phenylpropan-2-yl]-1-aryl-5-methyl-1H-1,2,3-triazole-4-formamide, through one-pot oriented synthesis method. After pre-liminary evaluation, the chiral triazoline-oxazoline ligands, in which 1,2,3-triazole rings, like pyridine-type rings, chiral materials were saved and replace one oxazoline ring in the dioxazoline ligands for asymmetric catalytic reactions.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"328 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141613041","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-05DOI: 10.2174/0115701794299562240606054510
Muhammad Shoaib Sardar, Shou-Jun Xu
Introduction:: The objective of this study is to compute the Kirchhoff index and re-sistance distance for two classes of windmill graphs, namely the French windmill graph and the Dutch windmill graph. Methods:: In this study, G is considered a simple connected graph with vertex set V (G) and edge set E(G). N is supposed to represent a network derived from G by substituting a 1-ohm resistor for each edge of G. In that case, the resistance between μ,ν ∈ V (G) is considered analogous to the resistance between two equivalent nodes in network N. Results:: The Kirchhoff index of G is the sum of the resistance distances between all pairs of vertices in G. Conclusion:: In addition, the Kirchhoff index and resistance distance are computed in this study for specific generalizations of these graphs.
导言本研究旨在计算两类风车图（即法国风车图和荷兰风车图）的基尔霍夫指数和重阻距离。方法：：在本研究中，G 被视为简单连通图，具有顶点集 V (G) 和边集 E(G)。在这种情况下，μ,ν ∈ V (G) 之间的电阻被认为类似于网络 N 中两个等效节点之间的电阻。结果：：G 的基尔霍夫指数是 G 中所有顶点对之间电阻距离的总和：此外，本研究还计算了这些图的特定广义的基尔霍夫指数和电阻距离。
{"title":"Resistance Distance and Kirchhoff Index in Windmill Graphs","authors":"Muhammad Shoaib Sardar, Shou-Jun Xu","doi":"10.2174/0115701794299562240606054510","DOIUrl":"https://doi.org/10.2174/0115701794299562240606054510","url":null,"abstract":"Introduction:: The objective of this study is to compute the Kirchhoff index and re-sistance distance for two classes of windmill graphs, namely the French windmill graph and the Dutch windmill graph. Methods:: In this study, G is considered a simple connected graph with vertex set V (G) and edge set E(G). N is supposed to represent a network derived from G by substituting a 1-ohm resistor for each edge of G. In that case, the resistance between μ,ν ∈ V (G) is considered analogous to the resistance between two equivalent nodes in network N. Results:: The Kirchhoff index of G is the sum of the resistance distances between all pairs of vertices in G. Conclusion:: In addition, the Kirchhoff index and resistance distance are computed in this study for specific generalizations of these graphs.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"6 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141547433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-04DOI: 10.2174/0115701794307242240612075648
Taha Jafari, Seyed Morteza Naghib, M. R. Mozafari
: The biopolymer chitosan, which is derived from chitin, has shown great promise for tissue regeneration and regulated drug delivery. Its broad-spectrum antibacterial action, low toxicity, biocompatibility, and many other attributes make it appealing for use in biomedical applications. Crucially, chitosan may be synthesized into a range of forms that can be customized to provide desired results, such as hydrogels, membranes, scaffolds, and nanoparticles. Hydrogels that are biocompatible and self-healing are innovative soft materials with considerable potential for use in biomedical applications. Hydrogels that self-heal using chitosan, which are mostly made by dynamic imine linkages, have gained a lot of interest because of their great biocompatibility, moderate preparation requirements, and capacity to mend themselves in a physiological setting. In this study, a summary of the applications of chitosan-based self-healing hydrogels in bone, cartilage, and tooth tissue regeneration and drug delivery is provided. Lastly, we have mentioned the difficulties and potential outcomes for the biomedical field's creation of hydrogels based on chitosan that can mend themselves.
{"title":"Chitosan-Based Nano/Biomaterials in Bone Tissue Engineering and Regenerative Medicine: Recent Progress and Advances","authors":"Taha Jafari, Seyed Morteza Naghib, M. R. Mozafari","doi":"10.2174/0115701794307242240612075648","DOIUrl":"https://doi.org/10.2174/0115701794307242240612075648","url":null,"abstract":": The biopolymer chitosan, which is derived from chitin, has shown great promise for tissue regeneration and regulated drug delivery. Its broad-spectrum antibacterial action, low toxicity, biocompatibility, and many other attributes make it appealing for use in biomedical applications. Crucially, chitosan may be synthesized into a range of forms that can be customized to provide desired results, such as hydrogels, membranes, scaffolds, and nanoparticles. Hydrogels that are biocompatible and self-healing are innovative soft materials with considerable potential for use in biomedical applications. Hydrogels that self-heal using chitosan, which are mostly made by dynamic imine linkages, have gained a lot of interest because of their great biocompatibility, moderate preparation requirements, and capacity to mend themselves in a physiological setting. In this study, a summary of the applications of chitosan-based self-healing hydrogels in bone, cartilage, and tooth tissue regeneration and drug delivery is provided. Lastly, we have mentioned the difficulties and potential outcomes for the biomedical field's creation of hydrogels based on chitosan that can mend themselves.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"51 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141552607","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-03DOI: 10.2174/0115701794310949240607113838
Jehan Y. Al-Humaidi, Sobhi M. Gomha, Lamia A. Albedair, Magdi E. A. Zaki, Yousef E. Mukhrish, Mahmoud A. Mohamed
Background: Given the inadequacies of current chemotherapy, there is a need for more effective anticancer agents. Imidazole and thiazole compounds have demonstrated significant biological activity, making them promising candidates. Aims and Objective: This study investigates the anticancer potential of imidazole and thiazole derivatives, focusing on liver cancer. The aim is to synthesize bis-imidazole-thiazole hybrids and evaluate their efficacy as anticancer agents against hepatocellular carcinoma. Methods: The hybrids were synthesized using (2,2'-((1,4-phenylenebis(2-mercapto-4-methyl1H-imidazole-1,5-diyl))bis(ethan-1-yl-1-ylidene))bis(hydrazine-1-carbothioamide), hydrazonoyl halides, and α-halo ketones, catalyzed by DABCO. This method is designed to be fast, yield high amounts of product, and be environmentally friendly. Structural confirmation was provided by FT IR, NMR, and MS spectroscopy. Results: The synthesized hybrids were tested in vitro against HepG-2 and WI-38 cell lines. Compounds 16b, 14a, 16a, and 7b showed significant inhibitory activity, with IC50 values indicating strong inhibition comparable to or better than the standard drug Sorafenib. Conclusion: The bis-imidazole-thiazole hybrids exhibit potent anticancer properties, particularly against hepatocellular carcinoma, making them potential candidates for future cancer therapies. Their selectivity and safety were further demonstrated by their effects on normal WI-38 human fibroblasts.
{"title":"Green Synthesis and Anticancer Activity of New Bis-Imidazole-Thiazole Hybrids Targeting Hepatocellular Carcinoma","authors":"Jehan Y. Al-Humaidi, Sobhi M. Gomha, Lamia A. Albedair, Magdi E. A. Zaki, Yousef E. Mukhrish, Mahmoud A. Mohamed","doi":"10.2174/0115701794310949240607113838","DOIUrl":"https://doi.org/10.2174/0115701794310949240607113838","url":null,"abstract":"Background: Given the inadequacies of current chemotherapy, there is a need for more effective anticancer agents. Imidazole and thiazole compounds have demonstrated significant biological activity, making them promising candidates. Aims and Objective: This study investigates the anticancer potential of imidazole and thiazole derivatives, focusing on liver cancer. The aim is to synthesize bis-imidazole-thiazole hybrids and evaluate their efficacy as anticancer agents against hepatocellular carcinoma. Methods: The hybrids were synthesized using (2,2'-((1,4-phenylenebis(2-mercapto-4-methyl1H-imidazole-1,5-diyl))bis(ethan-1-yl-1-ylidene))bis(hydrazine-1-carbothioamide), hydrazonoyl halides, and α-halo ketones, catalyzed by DABCO. This method is designed to be fast, yield high amounts of product, and be environmentally friendly. Structural confirmation was provided by FT IR, NMR, and MS spectroscopy. Results: The synthesized hybrids were tested in vitro against HepG-2 and WI-38 cell lines. Compounds 16b, 14a, 16a, and 7b showed significant inhibitory activity, with IC50 values indicating strong inhibition comparable to or better than the standard drug Sorafenib. Conclusion: The bis-imidazole-thiazole hybrids exhibit potent anticancer properties, particularly against hepatocellular carcinoma, making them potential candidates for future cancer therapies. Their selectivity and safety were further demonstrated by their effects on normal WI-38 human fibroblasts.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"20 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141547434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-02DOI: 10.2174/0115701794314387240604112621
Ebrahim Rezaii, Mehrdad Mahkam, Mohammad Rezaii
aims: Synthesis of organic-inorganic hybrids as 3D adsorbents for heavy metal removal background: Synthesis of organic-inorganic hybrids objective: Study of heavy metal removal with porous nanocomposite scaffolds based on hybrid organic/inorganic nanoparticles (MSN@COF) method: Using soluthermal methods for the synthesis of organic-inorganic hybrids and studying the removal of heavy metals in them result: Precise and defect-free synthesis of organic-inorganic hybrids Removal of over 90% of heavy metals conclusion: In this research work, in order to achieve the desired product, mesoporous silica nanoparticles were first synthesized based on TEOS, and then the surface modification of these nanoparticles was done with APTES in order to achieve MSN-NH2. Next, organic covalent frameworks based on cyanuric chloride were synthesized. The main goal in this research work was the synthesis of porous nanocomposites based on MSN and COF, so that it is possible to synthesize hybrid organic/inorganic porous nanocomposites by in situ growth of COF on porous silica nanoparticles. Therefore, after synthesizing both hybrid organic/inorganic porous nanocomposites (COF and MSN) and examining their morphology and how to identify them, porous nanocomposites (MSN@COF) resulting from the growth of COF on MSN were synthesized. To achieve a proper comparison of the porosity and nature of these nanocomposites, once this nanocomposite was synthesized using MSNs whose surfactant was not removed, the CTAB surfactant was removed after COF growth on it. In another synthesis, the nanocomposite was synthesized from the growth of COF on MSN-NH2 whose surfactant was removed. This nanocomposite, due to the open pores of the MSNs, the growth of COF started by connecting to the amino groups obtained from APTES from within the MSN-NH2 themselves. The nanocomposite had less porosity than the other composite due to the growth of COF inside it. But the remarkable thing was the growth and presence of COF with its constituent atoms inside the MSN cavities. Due to the fact that porous nanomaterials have their own unique morphology, nature, function, and application according to their constituents and porosity category, both porous nanoparticles used in the preparation of these nanocomposites are well-known and widely used porous nanomaterials. They are in industry and medicine, so we decided to synthesize porous nanocomposites that have the special characteristics, behavior, and ability of both MSN and COF. Relevant analyses confirmed the synthesis of these porous nano absorbents. The growth of COF on MSNs, according to the data obtained from BET, has reduced the surface area and volume of pores in porous nanocomposites, but on the other hand, the presence of COF with its constituent atoms definitely gives a special characteristic and ability to nanocomposites. Porous materials will give in exchange for a decrease in the surface area and volume of the initial MSN cavities. The results of thi
{"title":"Study of Heavy Metal Removal with Porous Nanocomposite Scaffolds based on Hybrid Inorganic/Organic Nanoparticles (MSN@COF)","authors":"Ebrahim Rezaii, Mehrdad Mahkam, Mohammad Rezaii","doi":"10.2174/0115701794314387240604112621","DOIUrl":"https://doi.org/10.2174/0115701794314387240604112621","url":null,"abstract":"aims: Synthesis of organic-inorganic hybrids as 3D adsorbents for heavy metal removal background: Synthesis of organic-inorganic hybrids objective: Study of heavy metal removal with porous nanocomposite scaffolds based on hybrid organic/inorganic nanoparticles (MSN@COF) method: Using soluthermal methods for the synthesis of organic-inorganic hybrids and studying the removal of heavy metals in them result: Precise and defect-free synthesis of organic-inorganic hybrids Removal of over 90% of heavy metals conclusion: In this research work, in order to achieve the desired product, mesoporous silica nanoparticles were first synthesized based on TEOS, and then the surface modification of these nanoparticles was done with APTES in order to achieve MSN-NH2. Next, organic covalent frameworks based on cyanuric chloride were synthesized. The main goal in this research work was the synthesis of porous nanocomposites based on MSN and COF, so that it is possible to synthesize hybrid organic/inorganic porous nanocomposites by in situ growth of COF on porous silica nanoparticles. Therefore, after synthesizing both hybrid organic/inorganic porous nanocomposites (COF and MSN) and examining their morphology and how to identify them, porous nanocomposites (MSN@COF) resulting from the growth of COF on MSN were synthesized. To achieve a proper comparison of the porosity and nature of these nanocomposites, once this nanocomposite was synthesized using MSNs whose surfactant was not removed, the CTAB surfactant was removed after COF growth on it. In another synthesis, the nanocomposite was synthesized from the growth of COF on MSN-NH2 whose surfactant was removed. This nanocomposite, due to the open pores of the MSNs, the growth of COF started by connecting to the amino groups obtained from APTES from within the MSN-NH2 themselves. The nanocomposite had less porosity than the other composite due to the growth of COF inside it. But the remarkable thing was the growth and presence of COF with its constituent atoms inside the MSN cavities. Due to the fact that porous nanomaterials have their own unique morphology, nature, function, and application according to their constituents and porosity category, both porous nanoparticles used in the preparation of these nanocomposites are well-known and widely used porous nanomaterials. They are in industry and medicine, so we decided to synthesize porous nanocomposites that have the special characteristics, behavior, and ability of both MSN and COF. Relevant analyses confirmed the synthesis of these porous nano absorbents. The growth of COF on MSNs, according to the data obtained from BET, has reduced the surface area and volume of pores in porous nanocomposites, but on the other hand, the presence of COF with its constituent atoms definitely gives a special characteristic and ability to nanocomposites. Porous materials will give in exchange for a decrease in the surface area and volume of the initial MSN cavities. The results of thi","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"2013 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141525345","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-26DOI: 10.2174/0115701794285586240523101245
Mohamad Hesam Shahrajabian, Wenli Sun
: Bitter melon (Momordica charantia L.) is a member of the Cucurbitaceae, which is also known as bitter squash, bitter gourd, karela, Goya melon and balsam pear. It is a rich source of different vitamins, potassium, zinc and other nutrients. The main pharmaceutical benefits of bitter melon are “antiinflammatory”, “antioxidant activity”, “antimicrobial characteristic”, “anticancer activity”, and “antihelmintic activity”, “antidiabetic effects”, “antiinflammation activity” and “treat skin conditions”. Its fruit is the main part of the plant which has been used for medicinal and food purposes. The primary metabolites in bitter gourd are common sugars, chlorophyll and proteins while secondary metabolites are carotenoids, alkaloids, phenolics, curcubitane triterpenoids, saponins, etc. The present review aims to study and survey on the nearly up-to-date results and findings regarding the pharmaceutical advantages and health benefits of bitter melon in an organic life.
{"title":"Multidimensional Uses of Bitter Melon (Momordica charantia L.) Considering the Important Functions of its Chemical Components","authors":"Mohamad Hesam Shahrajabian, Wenli Sun","doi":"10.2174/0115701794285586240523101245","DOIUrl":"https://doi.org/10.2174/0115701794285586240523101245","url":null,"abstract":": Bitter melon (Momordica charantia L.) is a member of the Cucurbitaceae, which is also known as bitter squash, bitter gourd, karela, Goya melon and balsam pear. It is a rich source of different vitamins, potassium, zinc and other nutrients. The main pharmaceutical benefits of bitter melon are “antiinflammatory”, “antioxidant activity”, “antimicrobial characteristic”, “anticancer activity”, and “antihelmintic activity”, “antidiabetic effects”, “antiinflammation activity” and “treat skin conditions”. Its fruit is the main part of the plant which has been used for medicinal and food purposes. The primary metabolites in bitter gourd are common sugars, chlorophyll and proteins while secondary metabolites are carotenoids, alkaloids, phenolics, curcubitane triterpenoids, saponins, etc. The present review aims to study and survey on the nearly up-to-date results and findings regarding the pharmaceutical advantages and health benefits of bitter melon in an organic life.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"21 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141502864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-24DOI: 10.2174/0115701794307025240521114902
Fatemeh Doraghi, Farzad Gilaninezhad, Somaye Karimian, Bagher Larijani, Mohammad Mahdavi
: Unsaturated pyrazolones can participate in organocatalytic reactions with various substrates to form spiro-cyclic pyrazolones, and fuzed-pyrazolone heterocycles. The present review describes progress since 2013 in the organocatalysis transformations of unsaturated pyrazolones. Pyrazolones are prevalent structural motifs in a wide variety of natural products and drug or drug-like molecules. A series of nitrogen-containing pyrazolones exhibits anti-cancer, antimicrobial, anti-inflammatory, anticonvulsant, antidepressant, antidiabetic, and an-tipyretic activities. Especially, chiral spiro-cyclic pyrazolones are recognized as targets in nat-ural products and clinical pharmaceuticals. Organocatalytic systems are powerful and reliable approaches that allow us to build structurally complex molecules in an enantioselectively and diastereoselectively manner. Avoiding the use of transition metal catalysts, readily available bifunctional organocatalysts, and the performance of the reaction at ambient temperature are other advantages of these catalytic systems. Despite considerable progress in this field, it is still one of the challenging goals for chemists to make new biologically active heterocyclic molecules.
{"title":"Developments in Organocatalysis Transformations of Unsaturated Pyrazolones","authors":"Fatemeh Doraghi, Farzad Gilaninezhad, Somaye Karimian, Bagher Larijani, Mohammad Mahdavi","doi":"10.2174/0115701794307025240521114902","DOIUrl":"https://doi.org/10.2174/0115701794307025240521114902","url":null,"abstract":": Unsaturated pyrazolones can participate in organocatalytic reactions with various substrates to form spiro-cyclic pyrazolones, and fuzed-pyrazolone heterocycles. The present review describes progress since 2013 in the organocatalysis transformations of unsaturated pyrazolones. Pyrazolones are prevalent structural motifs in a wide variety of natural products and drug or drug-like molecules. A series of nitrogen-containing pyrazolones exhibits anti-cancer, antimicrobial, anti-inflammatory, anticonvulsant, antidepressant, antidiabetic, and an-tipyretic activities. Especially, chiral spiro-cyclic pyrazolones are recognized as targets in nat-ural products and clinical pharmaceuticals. Organocatalytic systems are powerful and reliable approaches that allow us to build structurally complex molecules in an enantioselectively and diastereoselectively manner. Avoiding the use of transition metal catalysts, readily available bifunctional organocatalysts, and the performance of the reaction at ambient temperature are other advantages of these catalytic systems. Despite considerable progress in this field, it is still one of the challenging goals for chemists to make new biologically active heterocyclic molecules.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"81 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141502865","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-06DOI: 10.2174/0115701794259226231023091306
Ashraf H F Abd El-Wahab
In this work, a series of novel 3-(halophenyl)-1-phenyl-1H-pyrazole moieties have been synthesized. Their structures were characterized by IR, NMR, and MS spectroscopy, and the corresponding antitumor properties were also studied.
Objectives: This study aimed to synthesize a series of new 3-(halophenyl)-1-phenyl-1Hpyrazole moieties and survey the antitumor properties of these compounds.
Materials and methods: 3-(halophenyl)-1-phenyl-1H-pyrazoles (4a-j) were prepared by reaction of phenyl hydrazine (3) with different halogen aromatic aldehydes (1a-j) and malononitrile (2) in C2H5OH and piperidine. The reaction took place under microwave irradiation settings for two minutes at140°C.
Results: Three human cancer cell lines were used as in vitro test subjects for compounds 4a - j. Three cell lines from mammals HeLa (a cell line for human cervical cancer), MCF-7 (a cell line for human breast cancer), and PC-3 (a cell line for human prostate cancer), all with 5- fluorouracil as the standard reference drug were used.
Conclusion: A series of novel 3-(halophenyl)-1-phenyl-1H-pyrazoles were synthesized in this work. All substances had their anticancer properties assessed.
{"title":"Synthesis and Antitumor Activities of Novel 5-amino-3-(halophenyl)- 1- phenyl-1H-pyrazole-4-carbonitriles.","authors":"Ashraf H F Abd El-Wahab","doi":"10.2174/0115701794259226231023091306","DOIUrl":"https://doi.org/10.2174/0115701794259226231023091306","url":null,"abstract":"<p><p>In this work, a series of novel 3-(halophenyl)-1-phenyl-1H-pyrazole moieties have been synthesized. Their structures were characterized by IR, NMR, and MS spectroscopy, and the corresponding antitumor properties were also studied.</p><p><strong>Objectives: </strong>This study aimed to synthesize a series of new 3-(halophenyl)-1-phenyl-1Hpyrazole moieties and survey the antitumor properties of these compounds.</p><p><strong>Materials and methods: </strong>3-(halophenyl)-1-phenyl-1H-pyrazoles (4a-j) were prepared by reaction of phenyl hydrazine (3) with different halogen aromatic aldehydes (1a-j) and malononitrile (2) in C2H5OH and piperidine. The reaction took place under microwave irradiation settings for two minutes at140°C.</p><p><strong>Results: </strong>Three human cancer cell lines were used as in vitro test subjects for compounds 4a - j. Three cell lines from mammals HeLa (a cell line for human cervical cancer), MCF-7 (a cell line for human breast cancer), and PC-3 (a cell line for human prostate cancer), all with 5- fluorouracil as the standard reference drug were used.</p><p><strong>Conclusion: </strong>A series of novel 3-(halophenyl)-1-phenyl-1H-pyrazoles were synthesized in this work. All substances had their anticancer properties assessed.</p>","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140859693","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-04-24DOI: 10.2174/1570179421999240422115539
Manoj K. Jaiswal, Abhishek Gupta, Faisal J. Ansari, Vinay K. Pandey, Vinod K. Tiwari
Two errors appeared in the text of the manuscript titled “Recent Progress on Synthesis of Functionalized 1,5- disubstituted Triazoles”, 2024; 21(4) : 513-558 [1]. We regret the errors and apologize to readers. The original article can be found online at: https://www.eurekaselect.com/article/131107
标题为 "Recent Progress on Synthesis of Functionalized 1,5- disubstituted Triazoles"（《官能化 1,5-二取代三唑合成的最新进展》）的手稿文本中出现两处错误，2024; 21(4) : 513-558 [1]。我们对这些错误表示遗憾，并向读者致歉。原文可在线查阅： https://www.eurekaselect.com/article/131107
{"title":"Corrigendum to: Recent Progress on Synthesis of Functionalized 1,5- disubstituted Triazoles","authors":"Manoj K. Jaiswal, Abhishek Gupta, Faisal J. Ansari, Vinay K. Pandey, Vinod K. Tiwari","doi":"10.2174/1570179421999240422115539","DOIUrl":"https://doi.org/10.2174/1570179421999240422115539","url":null,"abstract":"Two errors appeared in the text of the manuscript titled “Recent Progress on Synthesis of Functionalized 1,5- disubstituted Triazoles”, 2024; 21(4) : 513-558 [1]. We regret the errors and apologize to readers. The original article can be found online at: https://www.eurekaselect.com/article/131107","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"51 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140799872","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-04-19DOI: 10.2174/0115701794291133240327044308
Dania Altaher, Hiba Zalloum, Kamal Sweidan, Dima A. Sabbah, Husam AlSalamat, Mahmoud Sunjuk, Reem Isleem
Introduction: A new series of 4-hydroxy-8-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide derivatives has been synthesized in good yields, followed by complete characteri-zation using 1D-NMR, 2D-NMR, and IR techniques. Methods:: The final products contain amide, hydroxyl, and aromatic functional groups that usu-ally show significant bioactivity. The target products have been examined towards three cancer cell lines, namely colorectal cancer cell line (HCT116), breast cancer cell line (MCF-7), and leukemia cell line (K562) in addition to the fibroblast cells, that were used as a model for normal human tissue. Results:: The anticancer results signified that compound 6 showed the most activity in the series accomplished with IC50 values of 14.6, 5.3 and 12.8 μM, Conclusion:: Other compounds exhibited considerable activity, such as compounds 9 (IC50 3.5 and 19.0 μM), 10 (IC50 12.6 μM), and 11 (IC50 10.3 μM) against the three cancer cell lines HCT116, MCF-7 and K562, respectively.
{"title":"Synthesis, Characterization and Preliminary Screening of New N-Substi-tuted -8-Methyl-4-Hydroxy-2-Quinolone -3-Carboxamides as Potential An-ticancer Agents","authors":"Dania Altaher, Hiba Zalloum, Kamal Sweidan, Dima A. Sabbah, Husam AlSalamat, Mahmoud Sunjuk, Reem Isleem","doi":"10.2174/0115701794291133240327044308","DOIUrl":"https://doi.org/10.2174/0115701794291133240327044308","url":null,"abstract":"Introduction: A new series of 4-hydroxy-8-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide derivatives has been synthesized in good yields, followed by complete characteri-zation using 1D-NMR, 2D-NMR, and IR techniques. Methods:: The final products contain amide, hydroxyl, and aromatic functional groups that usu-ally show significant bioactivity. The target products have been examined towards three cancer cell lines, namely colorectal cancer cell line (HCT116), breast cancer cell line (MCF-7), and leukemia cell line (K562) in addition to the fibroblast cells, that were used as a model for normal human tissue. Results:: The anticancer results signified that compound 6 showed the most activity in the series accomplished with IC50 values of 14.6, 5.3 and 12.8 μM, Conclusion:: Other compounds exhibited considerable activity, such as compounds 9 (IC50 3.5 and 19.0 μM), 10 (IC50 12.6 μM), and 11 (IC50 10.3 μM) against the three cancer cell lines HCT116, MCF-7 and K562, respectively.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"94 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140629863","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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