Category: 2682-49-7

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Synthetic and medicinal perspective of thiazolidinones: A review

In the modern scenario, thiazolidinone scaffold has emerged as a very potent scaffold as per its clinical significance concerned. It has attracted the keen interest of the researchers due to its great diversity in biological activities. Thiazolidinones are the saturated form of thiazole, called thiazolidine with a carbonyl group. The 1,3-thiazolidin-4-ones possess wide range of pharmacological activities such as anti-cancer, anti-diabetic, anti-microbial, anti-viral, anti-inflammatory and anti-convulsant. In the past few years, various newer synthetic approaches have been designed to synthesize diverse scaffolds to explore the various types of biological activities. In this review, an attempt has been made by the authors to summarize various synthetic strategies for thiazolidinone derivatives as well as their biological significance.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H337N | ChemSpider

Synthetic Route of 2682-49-7, One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time.In a article, authors is Ulusoy Guezeldemirci, Nuray, mentioned the application of Synthetic Route of 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS

Synthesis and antiviral activity evaluation of new 4-thiazolidinones bearing an imidazo[2,1-b]thiazole moiety

A series of new 4-thiazolidinone derivatives were synthesized and evaluated against diverse DNA- and RNA-viruses in mammalian cell cultures. Some of the compounds were found to exhibit moderate antiviral activity. 3-Propyl-2-[((6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-methyl-4-thiazolidinone 13, displayed modest yet consistent activity against three strains of influenza A virus, including the 2009 pandemic virus A/H1N1 Virginia/ATCC3/2009 (cytotoxicity >100 muM). Compounds 6 and 11 displayed activity against vesicular stomatitis virus in HeLa cells (antiviral EC50 values of 9 (cytotoxicity 100 muM) and 2 muM (cytotoxicity 20 muM), respectively). Neither of the compounds was active against HIV.

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2682-49-7, Name is Thiazolidin-2-one, belongs to thiazolidine compound, is a common compound. Computed Properties of C3H5NOSIn an article, once mentioned the new application about 2682-49-7.

Vanillin-related N-acylhydrazones: Synthesis, antischistosomal properties and target fishing studies

Background: Schistosomiasis is a neglected disease, which affects millions of people in developing countries. Its treatment relies on a single therapeutic alternative, the praziquantel. This situation may lead to drug resistance which, in turn, made urgent the need for new antischistosomal agents. N-acylhydrazones are usually explored as good antimicrobial agents, but the vanillin-related N-acylhydrazones have never been tested by their antiparasitic potential. Objective: Herein, we report the synthesis of seven analogues, three of them unpublished, their biological investigation against Schistosoma mansoni and Target Fishing studies. Methods: The compounds were synthesized following classical synthetical approaches. The anthelmintic potential was assessed as well as their cytotoxicity profile. Confocal laser scanning microscopy and target fishing study were performed to better understand the observed antischistosomal activity. Results: Compound GPQF-407 exhibited good antischistosomal activity (47.91 muM) with suitable selectivity index (4.14). Confocal laser scanning microscopy revealed that it triggered severe tegumental destruction and tubercle disintegration. Target fishing studies pointed out some probable targets, such as the serine-threonine kinases, dihydroorotate dehydrogenases and carbonic anhydrase II. Conclusion: The GPQF-407 was revealed to be a promising antischistosomal agent which, besides presenting the N-acylhydrazone privileged scaffold, also could be easily synthesized on large scales from commercially available materials.

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Electric Literature of 2682-49-7, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS. In a Article£¬once mentioned of 2682-49-7

One-pot synthesis of 4-thiazolidinone derivatives catalyzed by zinc acetate-schiff base complex immobilized on mesoporous molecular sieve MCM-41

A new simple and efficient one-pot synthesis of thiazolidinone derivatives via aldehydes, amines and mercaptoacetic acid in the presence of Zn(OAc)2-Schiff base complex immobilized on MCM-41 is described. A variety of aldehydes and amines were engaged in the study and afforded respective thiazolidinones in high yield (up to 98%). Moreover, consistent activity of recovered catalyst was found to be almost same up to five cycles in 80% yield.

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Related Products of 2682-49-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Hybridized quinoline derivatives as anticancer agents: Design, synthesis, biological evaluation and molecular docking

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

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Synthetic Route of 2682-49-7, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, Synthetic Route of 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery.

Carbazole scaffold in medicinal chemistry and natural products: A review from 2010-2015

9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H469N | ChemSpider

Electric Literature of 2682-49-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Design, synthesis and in-silico study of novel series of 2-phenyl- 3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one derivatives with potential anti-tubercular activity

In an attempt to identify potential new agents active against tuberculosis with Shikimate kinase as the target, a novel series of 2-phenyl- 3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one derivatives were synthesized by convenient one-pot three-component reaction of amine, aldehyde and mercaptoacetic acid on montmorillonite KSF clay as a solid acidic catalyst in good yields. The structures of the newly synthesized compounds were confirmed by IR, 1H-NMR and elemental analysis and were subjected for anti-tubercular activity by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv. Docking and ADMET studies were used to better describe the titled compounds as potential anti-tubercular agents. The compound, 2-(3,4-dimethoxyphenyl)-3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one(4j), was found to be the most active against Mycobacterium tuberculosis H37Rv with MIC of 1.6 mug/ml and good drug likeness and dock scores. Molecular docking study revealed that the molecules fit well into the cavity of Shikimate kinase. Also, the molecular properties and bioactivity scores for the synthesized compounds obtained by in-silico studies were found to be within the acceptable range defined for human use revealing their potential as possible drug-like compounds. The anti-tubercular activity of the titled compounds was comparable to that of the standard drug Isoniazid and Ciprofloxacin. The results indicate that the synthesized thiadiazolyl-thiazolidinone derivatives may have an affinity towards Shikimate kinase active site which can be further explored for selective target based studies. Thus these compounds could act as a potential lead for further anti-tubercular studies.

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Quinuclidine | C7H255N | ChemSpider

Reference of 2682-49-7, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, Reference of 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery.

An update on chemical classes targeting ERK1/2 for the management of cancer

Cancer, still in the limelight due to its dreadful nature, shows overexpression of multiple signaling macromolecules leading to failure of many chemotherapeutic agents and acquired resistance to chemotherapy. These factors highlight the significance of shifting toward targeted therapy in cancer research. Recently, ERKs (ERK1 and 2) have been established as a promising target for the management of various types of solid tumors, due to their aberrant involvement in cell growth and progression. Several ERKs inhibitors have reached clinical trials for the management of cancer and their derivatives are being continuously reported with noteworthy anticancer effect. This review highlights the recent reports on various chemical classes involved in the development of ERKs inhibitors along with their in vitro and in vivo activity and structure-activity relationship profile.

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Application of 2682-49-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. Application of 2682-49-7, Name is Thiazolidin-2-one,introducing its new discovery.

The bromodomain: From epigenome reader to druggable target

Lysine acetylation is a fundamental post-translational modification that plays an important role in the control of gene transcription in chromatin in an ordered fashion. The bromodomain, the conserved structural module present in transcription-associated proteins, functions exclusively to recognize acetyl-lysine on histones and non-histone proteins. The structural analyses of bromodomains’ recognition of lysine-acetylated peptides derived from histones and cellular proteins provide detailed insights into the differences and unifying features of biological ligand binding selectivity by the bromodomains. Newly developed small-molecule inhibitors targeting bromodomain proteins further highlight the functional importance of bromodomain/acetyl-lysine binding as a key mechanism in orchestrating molecular interactions and regulation in chromatin biology and gene transcription. These new studies argue that modulating bromodomain/acetyl-lysine interactions with small-molecule chemicals offer new opportunities to control gene expression in a wide array of human diseases including cancer and inflammation. This article is part of a Special Issue entitled: Molecular mechanisms of histone modification function.

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Synthesis, pharmacological evaluation and structure-activity relationship of recently discovered enzyme antagonist azoles

Global people are suffering from the legion of diseases. Cytotoxic property of the chemical compound would not solely influence effective drug properties and reduce unnecessary side effects. Proteins/enzymes responsible for microbe proliferation or survival are specifically targeted and inhibited successfully making the cells to undergo apoptosis. Furthermore, isoforms of essential enzymes have distinct physiological functions; thereby inhibition of essential enzyme isoforms is an apt way to the clinical approach of disease neutralization. Drugs are designed so as to play significant roles such as signaling pathways in the oncogenic process including cell proliferation, invasion, and angiogenesis. The present review comprises collective information of the recent synthesis of various organic drug compounds in brief, which could inhibit particular enzyme. The review also covers the correlation of the structure of a drug molecule designed and its inhibitory activity. Also, the most significant enzyme inhibitors are highlighted and structural moieties/core units responsible for remarkable inhibitory values are emphasized.Natural product chemistry; Organic chemistry; Enzyme inhibitors; Carbonic anhydrase; COX; Pyrazole; Thiazole

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