Pub Date : 2024-04-30DOI: 10.2174/0115701786303227240422140153
Amol R. Parhad, Dilip S. Aute, Anil G. Gadhave, Bhagwat K. Uphade
:: Our current work's primary goal is to create novel heterogeneous gallium sulfide (Ga2S3) nanocatalysts and investigate their catalytic activity in the synthesis of 3,3-(arylmethylene)-bis-(4- hydroxycoumarin) derivatives without use of solvent. FT-IR, XRD, SEM, and EDX analysis characterized the synthesized gallium sulfide (Ga2S3) nanomaterial catalysts. This method's main benefits are its short reaction time, solvent-free conditions, extremely mild reaction conditions, good product yield, and, most importantly, its ability to recover catalysts after at least four runs. background: Use nanocatalyst in multicomponent reaction. objective: To enhance the catalytic activity of nanocatalyst.
{"title":"Gallium Sulphide (Ga2S3): Green, Reusable, and Efficient Nanocatalyst for the Synthesis of 3,3-(arylmethylene)-bis-(4-hydroxycoumarin) Under Solvent-free Condition","authors":"Amol R. Parhad, Dilip S. Aute, Anil G. Gadhave, Bhagwat K. Uphade","doi":"10.2174/0115701786303227240422140153","DOIUrl":"https://doi.org/10.2174/0115701786303227240422140153","url":null,"abstract":":: Our current work's primary goal is to create novel heterogeneous gallium sulfide (Ga2S3) nanocatalysts and investigate their catalytic activity in the synthesis of 3,3-(arylmethylene)-bis-(4- hydroxycoumarin) derivatives without use of solvent. FT-IR, XRD, SEM, and EDX analysis characterized the synthesized gallium sulfide (Ga2S3) nanomaterial catalysts. This method's main benefits are its short reaction time, solvent-free conditions, extremely mild reaction conditions, good product yield, and, most importantly, its ability to recover catalysts after at least four runs. background: Use nanocatalyst in multicomponent reaction. objective: To enhance the catalytic activity of nanocatalyst.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"32 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140836863","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}
: A highly efficient and simple cross-coupling reaction of N-aryl aluminum reagents with Naryl thiosuccinimides for the synthesis of diarylsulide derivatives using CuCl (20 mol%) as a catalyst is reported. Under the optimum reaction conditions, the coupling reaction between aryl aluminum reagents with different substituents and N-aryl thiosuccinimides with different substituents can be carried out smoothly with 18-94% isolated yields of diarylsulides. The method avoids the use of expensive transition metals, such as Pd, Ir, or Rh, phosphine ligands, and has the advantages of simple operation and high reaction efficiency. The structures of all the target compounds are confirmed by 1 HNMR and 13CNMR.
{"title":"Ligand-Free, Copper-Catalyzed Coupling Reaction of Aryl Aluminum Reagents with N-Aryl Thiosuccinimides","authors":"Zhihao Zhang, Xiaoying Jia, Jiaxia Pu, Lirong Han, Jinsong Hou, Qinghan Li","doi":"10.2174/0115701786298931240408083720","DOIUrl":"https://doi.org/10.2174/0115701786298931240408083720","url":null,"abstract":": A highly efficient and simple cross-coupling reaction of N-aryl aluminum reagents with Naryl thiosuccinimides for the synthesis of diarylsulide derivatives using CuCl (20 mol%) as a catalyst is reported. Under the optimum reaction conditions, the coupling reaction between aryl aluminum reagents with different substituents and N-aryl thiosuccinimides with different substituents can be carried out smoothly with 18-94% isolated yields of diarylsulides. The method avoids the use of expensive transition metals, such as Pd, Ir, or Rh, phosphine ligands, and has the advantages of simple operation and high reaction efficiency. The structures of all the target compounds are confirmed by 1 HNMR and 13CNMR.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140624433","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 : 2024-04-17DOI: 10.2174/0115701786297846240408070836
Louchachha Isam, Edder Youssef, Faris Abdelmajid, Brahim Boualy, Mustapha Ait Ali, Abdallah Karim
: Dehydro-7,8-aryl-himachalene is a desired natural benzocycloheptene sesquiterpene found in the essential oil of Atlas cedar (Cedrus atlantica) in minor quantities. Herein, we report a simple and environmentally benign synthesis of this molecule via the aromatization of himachalene mixture (the major constituent of the same oil). The synthesis of the desired compound has been achieved by iodine/DMSO-mediated aromatization. The synthesized product has been characterized using MS spectrometry and NMR spectroscopy data. The treatment of the himachalene mixture with iodine led to the formation of dehydro-7,8-arylhimachalene, along with other rearrangement products catalyzed by the hydroiodic acid formed in situ. The use of DMSO as a co-solvent enabled the elimination of the acid formed and the regeneration of iodine. The optimization of the reaction conditions led to the formation of the desired product with a good yield. The present study highlights the development of a simple and environmentally benign method for the synthesis of a natural benzocycloheptene-based sesquiterpenoid in large quantities in order to explore its biological and chemical properties.
:脱氢-7,8-芳基-himachalene 是一种理想的天然苯并环庚烯倍半萜，可在阿特拉斯雪松（Cedrus atlantica）精油中少量发现。在此，我们报告了通过芳香化紫苏烯混合物（同一种精油的主要成分）合成这种分子的简单而环保的方法。我们通过碘/二甲基亚砜介导的芳香化反应合成了所需的化合物。利用 MS 光谱和 NMR 光谱数据对合成产物进行了表征。用碘处理桧烯混合物可生成脱氢-7,8-芳基桧烯，以及在原位形成的氢碘酸催化下的其他重排产物。使用二甲基亚砜作为助溶剂可以消除形成的酸，并使碘再生。通过优化反应条件，生成了所需的产物，而且收率很高。本研究强调了开发一种简单且对环境无害的方法，用于大量合成天然苯并环庚烯类倍半萜，以探索其生物和化学特性。
{"title":"Iodine-Mediated Aromatization of Himachalenes: Synthesis of Dehydro-7,8-arylhimachalene","authors":"Louchachha Isam, Edder Youssef, Faris Abdelmajid, Brahim Boualy, Mustapha Ait Ali, Abdallah Karim","doi":"10.2174/0115701786297846240408070836","DOIUrl":"https://doi.org/10.2174/0115701786297846240408070836","url":null,"abstract":": Dehydro-7,8-aryl-himachalene is a desired natural benzocycloheptene sesquiterpene found in the essential oil of Atlas cedar (Cedrus atlantica) in minor quantities. Herein, we report a simple and environmentally benign synthesis of this molecule via the aromatization of himachalene mixture (the major constituent of the same oil). The synthesis of the desired compound has been achieved by iodine/DMSO-mediated aromatization. The synthesized product has been characterized using MS spectrometry and NMR spectroscopy data. The treatment of the himachalene mixture with iodine led to the formation of dehydro-7,8-arylhimachalene, along with other rearrangement products catalyzed by the hydroiodic acid formed in situ. The use of DMSO as a co-solvent enabled the elimination of the acid formed and the regeneration of iodine. The optimization of the reaction conditions led to the formation of the desired product with a good yield. The present study highlights the development of a simple and environmentally benign method for the synthesis of a natural benzocycloheptene-based sesquiterpenoid in large quantities in order to explore its biological and chemical properties.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"58 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140613989","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}
: The acyl urea functionality and related analogs are increasingly used in medicinal chemistry and drug design to prove well-defined pharmacological actions and optimal physicochemical properties. This review paper aimed to summarize information related to synthesis methods of acyl urea derivatives, marketed products, and patents to explore their applications in counteracting CNS-related diseases by multiple targeting. Comprehensive data related to acyl urea and related compounds of the last 15 years is collected from various resources to provide enormous information to the readers. The content of the study uniformly includes considerable evidence linked to the common and unique synthesis techniques of acyl urea from starting materials like benzamide, isocyanates, substituted iodoglycals, 2 chloro nicotinic acid, and methyl hydrazines, as well as patents related to the same. This work describes the reactions of several substrates that can be used to manufacture various acyl urea derivatives. An understanding of patents related to acyl urea analogs with specific targets for CNS action may also help researchers working on additional synthesis of acyl urea derivatives with potential CNS action.
{"title":"An Insight into Common and Advanced Synthesis Methodologies of Acyl Urea Analogs Targeting the CNS","authors":"Preeti Kumari, Rakhi Mishra, Rupa Mazumder, Avijit Mazumder, Ayushi Singh, Gurvinder Singh, Pankaj Kumar Tyagi","doi":"10.2174/0115701786303718240409044341","DOIUrl":"https://doi.org/10.2174/0115701786303718240409044341","url":null,"abstract":": The acyl urea functionality and related analogs are increasingly used in medicinal chemistry and drug design to prove well-defined pharmacological actions and optimal physicochemical properties. This review paper aimed to summarize information related to synthesis methods of acyl urea derivatives, marketed products, and patents to explore their applications in counteracting CNS-related diseases by multiple targeting. Comprehensive data related to acyl urea and related compounds of the last 15 years is collected from various resources to provide enormous information to the readers. The content of the study uniformly includes considerable evidence linked to the common and unique synthesis techniques of acyl urea from starting materials like benzamide, isocyanates, substituted iodoglycals, 2 chloro nicotinic acid, and methyl hydrazines, as well as patents related to the same. This work describes the reactions of several substrates that can be used to manufacture various acyl urea derivatives. An understanding of patents related to acyl urea analogs with specific targets for CNS action may also help researchers working on additional synthesis of acyl urea derivatives with potential CNS action.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"29 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614058","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}
: Oxadiazole is an organic compound featuring a heterocyclic ring housing carbon, oxygen, and nitrogen atoms. Due to their heightened stability in biological environments, oxadiazole rings exhibit significant biological activities, effectively addressing health challenges like infectious diseases and chronic conditions in medicinal chemistry. The main objective of this review is to discuss various synthetic approaches related to 1,3,4-oxadiazole and its derivatives. The diverse reactivity positions oxadiazole as a valuable building block in organic synthesis, with derivatives exhibiting promising pharmacological activities. It involves a systematic literature review, critical analysis, and synthesis of existing research. This review comprises the ever-expanding chemical knowledge and has significant implications for drug development. Synthetic approaches to synthesizing oxadiazole through different schemes and methods have been discussed thoroughly. This review also concisely associated the pharmacological activities of oxadiazole and its derivatives. This review highlights the importance of continued research into the structure-activity relationships of oxadiazole derivatives, paving the way for developing novel and more potent therapeutic agents.
{"title":"Insight into the Novel Synthesis Approaches and Biological Activity of 1,3,4 Oxadiazole: A Review","authors":"Ayush Jain, Chandana Majee, Rupa Mazumder, Swrupanjali Padhi, Avijit Mazumder, Saumya Das, Arvind Kumar, Mvnl Chaitanya","doi":"10.2174/0115701786304096240324113413","DOIUrl":"https://doi.org/10.2174/0115701786304096240324113413","url":null,"abstract":": Oxadiazole is an organic compound featuring a heterocyclic ring housing carbon, oxygen, and nitrogen atoms. Due to their heightened stability in biological environments, oxadiazole rings exhibit significant biological activities, effectively addressing health challenges like infectious diseases and chronic conditions in medicinal chemistry. The main objective of this review is to discuss various synthetic approaches related to 1,3,4-oxadiazole and its derivatives. The diverse reactivity positions oxadiazole as a valuable building block in organic synthesis, with derivatives exhibiting promising pharmacological activities. It involves a systematic literature review, critical analysis, and synthesis of existing research. This review comprises the ever-expanding chemical knowledge and has significant implications for drug development. Synthetic approaches to synthesizing oxadiazole through different schemes and methods have been discussed thoroughly. This review also concisely associated the pharmacological activities of oxadiazole and its derivatives. This review highlights the importance of continued research into the structure-activity relationships of oxadiazole derivatives, paving the way for developing novel and more potent therapeutic agents.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140571279","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 : 2024-04-13DOI: 10.2174/0115701786294320240311022937
Nguyen Thi Chung, Vo Cong Dung, Dau Xuan Duc
: A facile and green strategy for the Knoevenagel condensation reaction of aryl aldehydes and active methylene compounds using [Bmim][CF3COO] ionic liquid as a solvent and a catalyst has been introduced. The method features some advantages, such as good to excellent yield of products, relatively short reaction time, mild reaction conditions, broad substrate scope, and scalability. Moreover, the ionic liquid solvent could be conveniently recycled and reused up to three times without any considerable loss of catalytic activity. Twelve products were obtained in high yields, and their structures were confirmed by NMR data. A plausible reaction mechanism involving the role of the ionic liquid catalyst was also suggested.
{"title":"[Bmim][CF3COO] as a Solvent and a Catalyst for the Knoevenagel Condensation","authors":"Nguyen Thi Chung, Vo Cong Dung, Dau Xuan Duc","doi":"10.2174/0115701786294320240311022937","DOIUrl":"https://doi.org/10.2174/0115701786294320240311022937","url":null,"abstract":": A facile and green strategy for the Knoevenagel condensation reaction of aryl aldehydes and active methylene compounds using [Bmim][CF3COO] ionic liquid as a solvent and a catalyst has been introduced. The method features some advantages, such as good to excellent yield of products, relatively short reaction time, mild reaction conditions, broad substrate scope, and scalability. Moreover, the ionic liquid solvent could be conveniently recycled and reused up to three times without any considerable loss of catalytic activity. Twelve products were obtained in high yields, and their structures were confirmed by NMR data. A plausible reaction mechanism involving the role of the ionic liquid catalyst was also suggested.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"50 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140571345","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 : 2024-04-09DOI: 10.2174/0115701786295452240327060732
Lay-Khoon Ong, Sie-Tiong Ha, Guan-Yeow Yeap, Siew-Ling Lee
:: New calamitic liquid crystals, 4-[{[4-(diethylamino)phenyl]methylidene}amino]phenyl 4- alkyloxybenzoate (nEABAA) containing mesogenic core system which made of three phenyl rings were reported. The ester and imine linkages connected the phenyl rings. At one end of the molecule, the core system was attached to an alkyloxy chain with a variable length -(CH2)n- (where n = 2-10, 12, 14, 16 and 18). At the other end of the molecule, the para position of the phenyl ring is bonded to the diethylamino group. The molecular structure of the current compounds was confirmed by using spectroscopic methods. The mesomorphic characteristics of the title compounds were studied by using a differential scanning calorimeter and a polarizing optical microscope attached to a heating stage. Through observation under microscopy, it was found that all synthesized compounds exhibited only a single (nematic) phase. The exhibition of the monophase variance (nematic) in the current compounds is caused by the presence of the diethylamino group that is attached to the terminal position of the benzylideneaniline core system. The diethylamino group has caused the molecular breadth to increase and this results in a weaker overall lateral intermolecular attraction. Subsequently, it depressed the mesophase thermal stability of the compounds. Thermal properties of the current compounds were compared with the earlier reported analogous and the structure-property relationships of the current compounds have been inferred through this comparison.
::新型钙钛矿液晶--4-[{[4-（二乙胺基）苯基]亚甲基}氨基]苯基 4-烷氧基苯甲酸酯（nEABAA）含有由三个苯基环组成的中生核心体系。酯和亚胺连接各苯基环。在分子的一端，核心系统连接着一条长度可变的烷氧基链-(CH2)n-（其中 n = 2-10、12、14、16 和 18）。在分子的另一端，苯环的对位键与二乙氨基相连。目前化合物的分子结构已通过光谱方法得到证实。利用差示扫描量热仪和安装在加热台上的偏光光学显微镜研究了标题化合物的介形特征。通过显微镜观察发现，所有合成化合物都只呈现出单（向列）相。目前的化合物之所以呈现单相（向列）变化，是因为在苄叉苯胺核心系统的末端位置附着了二乙氨基。二乙氨基基团导致分子宽度增加，从而减弱了分子间的整体横向吸引力。因此，这降低了化合物的介相热稳定性。我们将当前化合物的热性质与早先报道的类似化合物进行了比较，并通过比较推断出了当前化合物的结构-性质关系。
{"title":"Synthesis and Mesomorphism of New Calamitic Schiff Bases-Ester Possessing Dialkylamino Terminal Substituent","authors":"Lay-Khoon Ong, Sie-Tiong Ha, Guan-Yeow Yeap, Siew-Ling Lee","doi":"10.2174/0115701786295452240327060732","DOIUrl":"https://doi.org/10.2174/0115701786295452240327060732","url":null,"abstract":":: New calamitic liquid crystals, 4-[{[4-(diethylamino)phenyl]methylidene}amino]phenyl 4- alkyloxybenzoate (nEABAA) containing mesogenic core system which made of three phenyl rings were reported. The ester and imine linkages connected the phenyl rings. At one end of the molecule, the core system was attached to an alkyloxy chain with a variable length -(CH2)n- (where n = 2-10, 12, 14, 16 and 18). At the other end of the molecule, the para position of the phenyl ring is bonded to the diethylamino group. The molecular structure of the current compounds was confirmed by using spectroscopic methods. The mesomorphic characteristics of the title compounds were studied by using a differential scanning calorimeter and a polarizing optical microscope attached to a heating stage. Through observation under microscopy, it was found that all synthesized compounds exhibited only a single (nematic) phase. The exhibition of the monophase variance (nematic) in the current compounds is caused by the presence of the diethylamino group that is attached to the terminal position of the benzylideneaniline core system. The diethylamino group has caused the molecular breadth to increase and this results in a weaker overall lateral intermolecular attraction. Subsequently, it depressed the mesophase thermal stability of the compounds. Thermal properties of the current compounds were compared with the earlier reported analogous and the structure-property relationships of the current compounds have been inferred through this comparison.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"45 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140571283","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 : 2024-04-02DOI: 10.2174/0115701786286700240322065602
Sarah L. Wicks, Jake A. Roberts, Matthew J. Hurtt, Benjamin P. Hernandez, Jason J. Jones, Andrea L. Taylor, Jessica K. Logan, William J. Schreiber, Mouskudah G. Murray, Brandy L. Crenshaw, Craig B. Stevens, Robin K. Lammi, James M. Hanna Jr.
: Our group recently reported that the polyhydroxy aromatic compound 3,3′,4,4′- biphenyltetrol (2a) is a successful inhibitor of amyloid-β peptide (Aβ) aggregation, decreasing Aβ aggregation by 50 % when present in equimolar concentrations. In the present study, several additional biphenyltetrols were prepared and examined for their in vitro activity against aggregation of Aβ to investigate the effect of the relative positions of hydrogen-bond donors on the aggregation process. Congo red spectral shift assays demonstrated that, of the eight (8) additional biphenyltetrol compounds prepared, three (3) successfully inhibited the association of Aβ monomers, two symmetrical isomers, 2,2′,5,5′-biphenyltetrol (2c), and 2,2′,3,3′-biphenyltetrol (2d), along with one unsymmetrical isomer, 2,3′,4′,5-biphenyltetrol (2g). These results, along with the previously reported results of 2a, strongly suggest that hydroxyl group position affects the ability of the inhibitor to bind to Aβ assemblies, thus impacting inhibitory efficacy.
{"title":"Synthesis of Symmetrical and Unsymmetrical Tetrahydroxybiphenyls and their Evaluation as Amyloid-β Aggregation Inhibitors","authors":"Sarah L. Wicks, Jake A. Roberts, Matthew J. Hurtt, Benjamin P. Hernandez, Jason J. Jones, Andrea L. Taylor, Jessica K. Logan, William J. Schreiber, Mouskudah G. Murray, Brandy L. Crenshaw, Craig B. Stevens, Robin K. Lammi, James M. Hanna Jr.","doi":"10.2174/0115701786286700240322065602","DOIUrl":"https://doi.org/10.2174/0115701786286700240322065602","url":null,"abstract":": Our group recently reported that the polyhydroxy aromatic compound 3,3′,4,4′- biphenyltetrol (2a) is a successful inhibitor of amyloid-β peptide (Aβ) aggregation, decreasing Aβ aggregation by 50 % when present in equimolar concentrations. In the present study, several additional biphenyltetrols were prepared and examined for their in vitro activity against aggregation of Aβ to investigate the effect of the relative positions of hydrogen-bond donors on the aggregation process. Congo red spectral shift assays demonstrated that, of the eight (8) additional biphenyltetrol compounds prepared, three (3) successfully inhibited the association of Aβ monomers, two symmetrical isomers, 2,2′,5,5′-biphenyltetrol (2c), and 2,2′,3,3′-biphenyltetrol (2d), along with one unsymmetrical isomer, 2,3′,4′,5-biphenyltetrol (2g). These results, along with the previously reported results of 2a, strongly suggest that hydroxyl group position affects the ability of the inhibitor to bind to Aβ assemblies, thus impacting inhibitory efficacy.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"26 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140603168","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 : 2024-03-28DOI: 10.2174/0115701786292045240226050222
Animesh Mondal
:: The term isatin and its derivative-based MCRs have emerged over the years as a versatile, environment-friendly, and very promising platform for the construction of highly enabling bioactive organic scaffolds such as drugs, natural products, pharmaceuticals etc. In the world of recent advancements, the one-pot strategy based on isatin has come to the forefront of synthetic chemistry for the activation of small organic molecules. This present survey touched on the chemistry of isatin employed over the past decade to sketch and for the creation of various types of organic molecules consisting of heterocyclic or spiro-heterocyclic skeletons via one-pot methodology.
{"title":"A Brief Review Depending on the Chemistry of Isatin in Single Pot Technique Towards the Construction of Significant and Valuable Heterocyclic Scaffolds","authors":"Animesh Mondal","doi":"10.2174/0115701786292045240226050222","DOIUrl":"https://doi.org/10.2174/0115701786292045240226050222","url":null,"abstract":":: The term isatin and its derivative-based MCRs have emerged over the years as a versatile, environment-friendly, and very promising platform for the construction of highly enabling bioactive organic scaffolds such as drugs, natural products, pharmaceuticals etc. In the world of recent advancements, the one-pot strategy based on isatin has come to the forefront of synthetic chemistry for the activation of small organic molecules. This present survey touched on the chemistry of isatin employed over the past decade to sketch and for the creation of various types of organic molecules consisting of heterocyclic or spiro-heterocyclic skeletons via one-pot methodology.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"21 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140322259","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}
: Two polymer particles have been prepared by the reaction of N, N, N', N'-tetrakis(4- aminophenyl)-1,4-benzenediamine, 4, 4-biphenyldialdehyde and isophthalaldehyde, and characterized by SEM, FTIR and XRD. Based on methylene blue as the model pollutant, the adsorption properties of two polymer particles have been observed by using different adsorbent dosages, adsorption times and adsorption temperatures. Experimental data show that the removal rates of methylene blue wastewater are 74 % for polymer A and 68 % for polymer B, and the removal rates are up to 84% for polymer A and 74 % for polymer B after photo-catalytic treatment. All these suggest that the adsorption performance of polymer A is more excellent than that of polymer B. In addition, the methylene blue adsorption of the two Schiff base products conforms to the Freundlich adsorption isothermal model.
:通过 N, N, N', N'-tetrakis(4- aminophenyl)-1,4-benzenediamine, 4, 4-biphenylldialdehyde 和 isophthalaldehyde 反应制备了两种聚合物颗粒，并通过扫描电镜、傅立叶变换红外光谱和 XRD 进行了表征。以亚甲基蓝为模型污染物，采用不同的吸附剂用量、吸附时间和吸附温度，观察了两种聚合物颗粒的吸附性能。实验数据表明，聚合物 A 和聚合物 B 对亚甲蓝废水的去除率分别为 74% 和 68%，而经过光催化处理后，聚合物 A 和聚合物 B 的去除率分别高达 84% 和 74%。此外，两种席夫碱产品对亚甲基蓝的吸附均符合弗伦德里希吸附等温模型。
{"title":"Preparation and Adsorption Properties of Polymer Particles based on N, N, N', N'-Tetrakis(4-aminophenyl)-1,4-Benzenediamine","authors":"Jian-Yu Huang, Yong Liu, Ting-Hong Huang, Sheng-Zhi Liu, Ai-Ling Wu","doi":"10.2174/0115701786291281240318041709","DOIUrl":"https://doi.org/10.2174/0115701786291281240318041709","url":null,"abstract":": Two polymer particles have been prepared by the reaction of N, N, N', N'-tetrakis(4- aminophenyl)-1,4-benzenediamine, 4, 4-biphenyldialdehyde and isophthalaldehyde, and characterized by SEM, FTIR and XRD. Based on methylene blue as the model pollutant, the adsorption properties of two polymer particles have been observed by using different adsorbent dosages, adsorption times and adsorption temperatures. Experimental data show that the removal rates of methylene blue wastewater are 74 % for polymer A and 68 % for polymer B, and the removal rates are up to 84% for polymer A and 74 % for polymer B after photo-catalytic treatment. All these suggest that the adsorption performance of polymer A is more excellent than that of polymer B. In addition, the methylene blue adsorption of the two Schiff base products conforms to the Freundlich adsorption isothermal model.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":"16 1","pages":""},"PeriodicalIF":0.8,"publicationDate":"2024-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140300190","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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