Literature DB >> 33465668

Synthesis, anti-inflammatory and analgesic evaluation of thiazole/oxazole substituted benzothiazole derivatives.

Gajendra Kumar1, N P Singh2.   

Abstract

Non-Steroidal biologically active heterocyclic compounds 4-(2-(4-chlorophenyl) benzo[d]thiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo[d]thiazol-2-yl)methylene) thiazol-2-amine (3a-3d), 4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)-N-((3-substituted - 2-hydrobenzo [d]thiazol-2-yl)methylene)oxazol-2-amine (3a'-3d'), (Z)-N'-(4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)thiaol-2-yl)-N-(4-substituted phenylimino)-3-substituted-2-hydrobenzo[d]thiazole-2-carboxamidine (4a-4 h) and (Z)-N'-(4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)oxazol-2-yl)-N-(4-substituted phenylimino) - 3-substituted-2-hydrobenzo[d]thiazole-2-carboxamidine (4a'-4h') were synthesized starting from 2-chloro-1-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl) ethanone (1). The structure configuration of newly synthesized compounds has been determined by elemental analysis and various spectroscopic (IR, 1HNMR and GCMS) techniques. These compounds were tested for their anti-inflammation, analgesic, ulcerogenic, acute toxicity and free radical scavenging action and compared with reference drugs in albino rats. Compound 4-(2-(4-chlorophenyl)benzo[d]thiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo [d]thiazol-2-yl)methylene)thiazol-2-amine (3c) was the most active compound than reference drug at a dose of 50 mg/kg p.o.
Copyright © 2020 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Acute toxicity; Analgesic; Anti-inflammation; Benzothiazole; Free radical scavenging; Oxazole; Thiazole; Ulcerogenic

Year:  2020        PMID: 33465668     DOI: 10.1016/j.bioorg.2020.104608

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  4 in total

1.  Benzothiazole and Chromone Derivatives as Potential ATR Kinase Inhibitors and Anticancer Agents.

Authors:  Mykhaylo Frasinyuk; Dimple Chhabria; Victor Kartsev; Haritha Dilip; Samvel N Sirakanyan; Sivapriya Kirubakaran; Anthi Petrou; Athina Geronikaki; Domenico Spinelli
Journal:  Molecules       Date:  2022-07-20       Impact factor: 4.927

2.  Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors.

Authors:  Azhar O El-Abd; Said M Bayomi; Ashraf K El-Damasy; Basem Mansour; Naglaa I Abdel-Aziz; Magda A El-Sherbeny
Journal:  ACS Omega       Date:  2022-09-07

3.  Novel Thiophene Thioglycosides Substituted with the Benzothiazole Moiety: Synthesis, Characterization, Antiviral and Anticancer Evaluations, and NS3/4A and USP7 Enzyme Inhibitions.

Authors:  Rasha A Azzam; Nagwa M Gad; Galal H Elgemeie
Journal:  ACS Omega       Date:  2022-09-29

4.  Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation.

Authors:  Christophe Tratrat; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Marina Kostić; Marina Soković; Ioannis S Vizirianakis; Nikoleta F Theodoroula; Michelyne Haroun
Journal:  Molecules       Date:  2022-03-16       Impact factor: 4.411

  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.