scholarly journals Chemistry, synthesis and progress report on biological activities of thiadiazole compounds - a review

2016 ◽  
Vol 5 (5) ◽  
pp. 568-588
Author(s):  
Mohammad Asif
Keyword(s):  
Heterocyclic Compounds ◽  
Chelating Agents ◽  
Biological Activities ◽  
Progress Report ◽  
Biological Applications ◽  
Efficacy And Safety ◽  
Metal Chelating ◽  
Structure Activity ◽  
Oxidation Inhibitors ◽  
Relationship Of

Thiadiazoles are an important class of heterocyclic compounds that exhibit diverse applications in organic synthesis, pharmaceutical and biological applications. They are also useful as oxidation inhibitors, cyanine dyes, metal chelating agents, anti-corrosion agents. Researchers across the globe are working on this moiety due to their broad spectrum of applications of thiadiazole chemistry. This article provides information about developments, exploration, synthetic strategies, techniques for the synthesis of thiadiazoles and their diverse biological activities, structure-activity relationship of the compounds and physical properties. This article is an important tool for organic and medicinal chemists to develop newer thiadiazole compounds that could be better agents in terms of efficacy and safety.

Single Heterocyclic Compounds as Monoamine Oxidase Inhibitors: From Past to Present

2020 ◽  
Vol 20 (10) ◽  
pp. 908-920 ◽  
Author(s):  
Su-Min Wu ◽  
Xiao-Yang Qiu ◽  
Shu-Juan Liu ◽  
Juan Sun
Keyword(s):  
Monoamine Oxidase ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
The Past ◽  
Structure Activity ◽  
Receptor Interactions ◽  
Heterocyclic Derivatives ◽  
Inhibitory Activities ◽  
Leading Compounds ◽  
Heterocyclic Moiety

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson’s disease and Alzheimer’s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.

Antinociceptive Activity and Preliminary Structure-Activity Relationship of Chalcone-Like Compounds

2008 ◽  
Vol 63 (11-12) ◽  
pp. 830-836 ◽  
Author(s):  
Rogério Corrêa ◽  
Bruna Proiss Fenner ◽  
Fátima de Campos Buzzi ◽  
Valdir Cechinel Filho ◽  
Ricardo José Nunes
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Experimental Models ◽  
Antinociceptive Activity ◽  
Dominant Factor ◽  
Writhing Test ◽  
Aromatic Ketones ◽  
Structure Activity ◽  
Relationship Of

Abstract Chalcones belong to a class of α,β unsaturated aromatic ketones which occur abundantly in nature, especially in plants. They are promising and interesting compounds due to their vast applications in pharmaceuticals, agriculture and industry. Several studies have shown that these compounds exert important biological activities in different experimental models. The present work deals with the antinociceptive activity, evaluated against the writhing test, of three series of chalcone-like compounds obtained by the Claisen-Schmidt condensation, using different aldehydes and substituted acetophenones. The results reveal that the compounds synthesized show a significant antinociceptive effect compared with nonsteroidal drugs such as aspirin, paracetamol and diclofenac. They also show that the electronic demand of the substituents is the dominant factor of the biological activity.

scholarly journals Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 3036
Author(s):  
Ashraf A. Aly ◽  
Alaa A. Hassan ◽  
Maysa M. Makhlouf ◽  
Stefan Bräse
Keyword(s):  
Natural Products ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Biological Applications ◽  
Active Moiety ◽  
Interesting Class

Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

Aurones as New Porcine Pancreatic α-Amylase Inhibitors

2019 ◽  
Vol 16 (3) ◽  
pp. 333-340
Author(s):  
Khashayar Roshanzamir ◽  
Elaheh Kashani-Amin ◽  
Azadeh Ebrahim-Habibi ◽  
Latifeh Navidpour
Keyword(s):  
Biological Activities ◽  
Structural Isomers ◽  
Structural Requirements ◽  
Oh Groups ◽  
Structure Activity ◽  
Inhibitory Activities ◽  
Pharmacological Potential ◽  
Relationship Of ◽  
Amylase Inhibitors

Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturallyoccurring structural isomers of flavones, with promising pharmacological potential. </P><P> Methods: In this study, the structural requirements for the inhibition of porcine pancreatic &#945;- amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic &#945;-amylase. </P><P> Results: The structure-activity relationship of these inhibitors based on both in vitro and in silico findings showed that the hydrogen bonds between the OH groups of the A or B ring of (Z)- benzylidenebenzofuran-3-one derivatives and the catalytic residues of the binding site are crucial for their inhibitory activities. </P><P> Conclusion: It seems that the OH groups in aurones inhibit &#945;-amylase in a manner similar to that of OH groups in flavones and flavonols.

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications

2020 ◽  
Vol 20 ◽  
Author(s):  
Jinling Qin ◽  
Weyland Cheng ◽  
Yong-Tao Duan ◽  
Hua Yang ◽  
Yongfang Yao
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Vital Role ◽  
Drug Molecules ◽  
Structure Activity ◽  
Privileged Scaffold ◽  
Future Direction ◽  
Relationship Of ◽  
Anti Hiv ◽  
Clinical Drug

Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemicalcompound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compoundswhere the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

scholarly journals Structure-activity relationship of swainsonine. Inhibition of human α-mannosidases by swainsonine analogues

1989 ◽  
Vol 259 (3) ◽  
pp. 855-861 ◽  
Author(s):  
I Cenci di Bello ◽  
G Fleet ◽  
S K Namgoong ◽  
K I Tadano ◽  
B Winchester
Keyword(s):  
Biological Activities ◽  
Human Fibroblasts ◽  
Appreciable Effect ◽  
Open Chain ◽  
Structure Activity ◽  
Competitive Inhibitors ◽  
Storage Products ◽  
Glycoprotein Processing ◽  
Relationship Of

The inhibitory properties of a series of synthetic epimers and analogues of swainsonine towards the multiple forms of human alpha-mannosidases were studied in vitro and in cells in culture. Of the five epimers tested, only the 8a-epimer and 8,8a-diepimer of swainsonine were specific and competitive inhibitors (Ki values of 7.5 x 10(-5) and 2 x 10(-6) M respectively) of lysosomal alpha-mannosidases in vitro and induced storage of mannose-rich oligosaccharides in human fibroblasts in culture. The structures of these storage products indicated that processing alpha-mannosidases had also been inhibited. This was consistent with the observed inhibition in vitro of these enzymes by these compounds. In contrast, the 8-epimer, 1,8-diepimer and 2,8a-diepimer of swainsonine had no appreciable effect on any alpha-mannosidases. The corresponding open-chain analogues of swainsonine, namely 1,4-dideoxy-1,4-imino-D-mannitol, of the 8a-epimer, namely 1,4-dideoxy-1,4-imino-D-talitol, and of the 8,8a-diepimer, namely 1,4-dideoxy-1,4-imino-L-allitol, were weaker competitive inhibitors of lysosomal alpha-mannosidase, with Ki values of 1.3 x 10(-5), 1.2 x 10(-4) and 1.2 x 10(-4) M respectively. These analogues also proved less effective at inducing oligosaccharide accumulation and in disturbing glycoprotein processing. These compounds offer the opportunity to determine which alterations in the chirality of the swainsonine molecule affect its inhibitory specificity. A comparison of their biological activities has identified reagents that will be useful for studying steps in the biosynthesis and catabolism of glycoproteins and that may be of potential value in chemotherapy.

Fused azolo-quinoxalines: Candidates for Medicinal Chemistry. A review of their biological applications

2020 ◽  
Vol 27 ◽  
Author(s):  
Cindy Patinote ◽  
Natalina Cirnat ◽  
Pierre-Antoine Bonnet ◽  
Carine Deleuze-Masquéfa
Keyword(s):  
Drug Delivery ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Extensive Literature ◽  
Biological Applications ◽  
Huge Amount ◽  
Bond Forming ◽  
Azole Ring ◽  
Available Information

: Heterocyclic compounds hold a huge and recognized place in the field of medicinal chemistry thanks to their multiple biological activities. Their synthetic pathways allow their easy and rapid access due to different bond forming methodologies and provide a huge amount of multi-functionalized compounds for drug delivery. The syntheses of heterocyclic compounds are today well known for the majority, described and reviewed in an extensive literature. In this review, we choose to gather and classify available information concerning the biological activities of quinoxaline-based compounds annulated at bond a containing one and more nitrogen atoms in the fused azole ring.

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