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}
Pub Date : 2024-04-16DOI: 10.2174/0115701794298435240324175513
Arman Seifallahi Teymourlouei, Seyed Morteza Naghib, M. R. Mozafari
:: Natural polysaccharide-based nanoparticles are known for their non-toxic nature and diverse medical applications. Graphene oxide (GO) nanoparticles show potential in cancer treat-ment due to their ability to target medication delivery and influence ROS generation. These nanocomposites are versatile in gene transport, therapy, and photodynamic therapy, especially when surface-modified. Proper dispersion and functionalization of GO in polymer matrices are crucial, with examples like hyaluronic acid-functionalized GO offering versatile platforms for cancer drug administration. The potential of graphene oxide extends to cancer phototherapy, electronic nanowires, hydrogels, antibacterial nanocomposites, and environmental applications. When activated by polysaccharides, graphene-based nanocomposites exhibit anti-inflammatory and anticancer properties, making them valuable across various industries, including water treat-ment.
{"title":"Stimuli-responsive Graphene-Polysaccharide Nanocomposites for Drug Delivery and Tissue Engineering","authors":"Arman Seifallahi Teymourlouei, Seyed Morteza Naghib, M. R. Mozafari","doi":"10.2174/0115701794298435240324175513","DOIUrl":"https://doi.org/10.2174/0115701794298435240324175513","url":null,"abstract":":: Natural polysaccharide-based nanoparticles are known for their non-toxic nature and diverse medical applications. Graphene oxide (GO) nanoparticles show potential in cancer treat-ment due to their ability to target medication delivery and influence ROS generation. These nanocomposites are versatile in gene transport, therapy, and photodynamic therapy, especially when surface-modified. Proper dispersion and functionalization of GO in polymer matrices are crucial, with examples like hyaluronic acid-functionalized GO offering versatile platforms for cancer drug administration. The potential of graphene oxide extends to cancer phototherapy, electronic nanowires, hydrogels, antibacterial nanocomposites, and environmental applications. When activated by polysaccharides, graphene-based nanocomposites exhibit anti-inflammatory and anticancer properties, making them valuable across various industries, including water treat-ment.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"203 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570462","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 : 2024-04-15DOI: 10.2174/0115701794294862240322040633
Luana A. Machado, Cynthia L. M. Pereira, Ana Clara G. de Souza, Elivelton A. Ferreira, Flávia F. C. Marques, Ednilsom Orestes, Maria H. Araujo, Karen L. R. Paiva, Marina S. Mesquita, Sônia N. Báo, Leandro F. Pedrosa, Muhammad Jawad Nasim, Claus Jacob, Eufrânio N. da SilvaJúnior
Introduction: Lipid droplets (LDs) serve as primary storage sites for neutral lipids within cells and are crucial for lipid metabolism. Disorders affecting LDs can contribute to the pathogenesis of common metabolic diseases such as obesity and can-cer, highlighting the importance of comprehending LD biology in health and disease contexts. background: Several synthetic methods for the preparation of BODIPYs are reported in the literature, yet the exploration of the different applications of this exciting class of fluorescent compounds is less studied and, therefore, a wide avenue of possibilities remains to be discovered. Methods: Fluorescence assays are commonly used for the detection and quantification of lipids in biological samples or lipid-rich environments. In this study, BODIPYs were synthesized and analyzed for structural confirmation. objective: synthesis of BODIPYs and evaluation of their affinity for intracellular lipid droplets Results: These compounds were subsequently evaluated for photophysical, electro-chemical (cyclic voltammetry) and theoretical analysis, followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. method: In this study, BODIPYs were synthesized and analyzed for structural confirmation. These compounds were subsequently evaluated for photophysical, electrochemical (cyclic voltammetry) and theoretical analysis followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. Conclusion: BODIPYs have been identified as fluorogenic probes for live-cell imag-ing studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets. result: BODIPYs have been identified as fluorogenic probes for live-cell imaging studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets.
{"title":"BODIPYs as Fluorogenic Probes for Live-Cell Imaging of Lipid Droplets: Photophysical and Computational Studies","authors":"Luana A. Machado, Cynthia L. M. Pereira, Ana Clara G. de Souza, Elivelton A. Ferreira, Flávia F. C. Marques, Ednilsom Orestes, Maria H. Araujo, Karen L. R. Paiva, Marina S. Mesquita, Sônia N. Báo, Leandro F. Pedrosa, Muhammad Jawad Nasim, Claus Jacob, Eufrânio N. da SilvaJúnior","doi":"10.2174/0115701794294862240322040633","DOIUrl":"https://doi.org/10.2174/0115701794294862240322040633","url":null,"abstract":"Introduction: Lipid droplets (LDs) serve as primary storage sites for neutral lipids within cells and are crucial for lipid metabolism. Disorders affecting LDs can contribute to the pathogenesis of common metabolic diseases such as obesity and can-cer, highlighting the importance of comprehending LD biology in health and disease contexts. background: Several synthetic methods for the preparation of BODIPYs are reported in the literature, yet the exploration of the different applications of this exciting class of fluorescent compounds is less studied and, therefore, a wide avenue of possibilities remains to be discovered. Methods: Fluorescence assays are commonly used for the detection and quantification of lipids in biological samples or lipid-rich environments. In this study, BODIPYs were synthesized and analyzed for structural confirmation. objective: synthesis of BODIPYs and evaluation of their affinity for intracellular lipid droplets Results: These compounds were subsequently evaluated for photophysical, electro-chemical (cyclic voltammetry) and theoretical analysis, followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. method: In this study, BODIPYs were synthesized and analyzed for structural confirmation. These compounds were subsequently evaluated for photophysical, electrochemical (cyclic voltammetry) and theoretical analysis followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. Conclusion: BODIPYs have been identified as fluorogenic probes for live-cell imag-ing studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets. result: BODIPYs have been identified as fluorogenic probes for live-cell imaging studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"60 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570464","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}
Introduction: The effect of power and duration of ultrasonic irradiation on the syn-thesis of thiazoles via the Hantzsch reaction was investigated. Methods: The reaction of phenacyl bromides with thioamides under ultrasonic irradiation af-forded the target thiazoles in good yields. Results: The results showed that high power and long irradiation time cause the decomposition of the reaction materials, and for this reaction, the irradiation power of 720 watts and a total duration of 4 minutes, wherein a pulsing function was performed in 50% of each second, were considered the most suitable irradiation properties for the synthesis of thiazoles through the Hantzsch reaction. Conclusion: The use of mild conditions, short time frame, high yields, simple separation of the reaction product, and no use of the base for neutralization are the advantages of the present method.
{"title":"Investigation of the Effect of Power and Duration of Ultrasonic Irradiation on the Synthesis of Thiazoles","authors":"Eghlima Ehsani, Afshin Sarvary, Setareh Habibzadeh","doi":"10.2174/0115701794287558240220115823","DOIUrl":"https://doi.org/10.2174/0115701794287558240220115823","url":null,"abstract":"Introduction: The effect of power and duration of ultrasonic irradiation on the syn-thesis of thiazoles via the Hantzsch reaction was investigated. Methods: The reaction of phenacyl bromides with thioamides under ultrasonic irradiation af-forded the target thiazoles in good yields. Results: The results showed that high power and long irradiation time cause the decomposition of the reaction materials, and for this reaction, the irradiation power of 720 watts and a total duration of 4 minutes, wherein a pulsing function was performed in 50% of each second, were considered the most suitable irradiation properties for the synthesis of thiazoles through the Hantzsch reaction. Conclusion: The use of mild conditions, short time frame, high yields, simple separation of the reaction product, and no use of the base for neutralization are the advantages of the present method.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"109 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570378","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}
Background:: Nowadays, macrocyclic compounds constitute a privileged source for the development of compounds with interesting biological properties. Ring-closing olefin me-tathesis has received great attention for the synthesis of small, medium, and larger ring systems. Methods:: In the present work, we described the synthesis of eight original pyridyl macrocyclic triarylmethanes using an efficient 3-step synthetic strategy. The bisalkylated 4,4'-(pyridin-X-ylmethylene) diphenols (X=2-4) were prepared by ring-closing metathesis as macrocyclization key step, using Grubbs second generation catalyst. Results:: The pyridyl macrocyclic triarylmethanes were obtained with moderate to good yields. The introduction of a pyridine N-oxide moiety before the macrocyclization proved to be interest-ing to afford a higher yield of the corresponding metathesis product. FT-IR, 1 H NMR, 13C NMR, and X-ray diffraction analysis have been used for the characterization of the synthesized compounds. Conclusion:: The synthetic strategy used here proposes an efficient alternative to prepare macro-cyclic triarylmethanes of different sizes.
背景如今，大环化合物是开发具有有趣生物特性的化合物的重要来源。在合成小环、中环和大环系统方面，闭环烯烃甲基化反应备受关注。方法：：在本研究中，我们采用高效的三步合成策略合成了 8 个原创的吡啶基大环三芳基甲烷。使用格拉布斯第二代催化剂，通过闭环偏析作为大环化关键步骤，制备了双烷基化的 4,4'-（吡啶-X-基亚甲基）二苯酚（X=2-4）。结果获得了中等至良好收率的吡啶基大环三芳基甲烷。事实证明，在大环化之前引入吡啶 N-氧化物分子，可以获得更高产率的相应偏合成产物。傅立叶变换红外光谱、1 H NMR、13C NMR 和 X 射线衍射分析被用于表征合成的化合物。结论本文采用的合成策略为制备不同尺寸的大环三芳基甲烷提供了一种有效的替代方法。
{"title":"Novel Pyridyl Macrocyclic Triarylmethanes: Synthesis by Ring-closing Metathesis and Chemical Analysis","authors":"Ameni Hadj Mohamed, Corinne Coutant, Moncef Msaddek, Maité Sylla-Iyarreta Veitía","doi":"10.2174/0115701794249707230930113307","DOIUrl":"https://doi.org/10.2174/0115701794249707230930113307","url":null,"abstract":"Background:: Nowadays, macrocyclic compounds constitute a privileged source for the development of compounds with interesting biological properties. Ring-closing olefin me-tathesis has received great attention for the synthesis of small, medium, and larger ring systems. Methods:: In the present work, we described the synthesis of eight original pyridyl macrocyclic triarylmethanes using an efficient 3-step synthetic strategy. The bisalkylated 4,4'-(pyridin-X-ylmethylene) diphenols (X=2-4) were prepared by ring-closing metathesis as macrocyclization key step, using Grubbs second generation catalyst. Results:: The pyridyl macrocyclic triarylmethanes were obtained with moderate to good yields. The introduction of a pyridine N-oxide moiety before the macrocyclization proved to be interest-ing to afford a higher yield of the corresponding metathesis product. FT-IR, 1 H NMR, 13C NMR, and X-ray diffraction analysis have been used for the characterization of the synthesized compounds. Conclusion:: The synthetic strategy used here proposes an efficient alternative to prepare macro-cyclic triarylmethanes of different sizes.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"57 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570458","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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