4.7 Article

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

Journal

BIOORGANIC CHEMISTRY
Volume 107, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104608

Keywords

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

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Various non-steroidal biologically active heterocyclic compounds were synthesized and tested for their activities, with compound 4-(2-(4-chlomphenyebenzoldlthiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo [d] thiazol-2-yl)methylene)thiazol-2-amine (3c) showing the highest activity compared to reference drugs.
Non-Steroidal biologically active heterocyclic compounds 4 (2-(4-chlorophenyl) benzo [d] thiazol-3(2H)-yl)-N-((3-substituted-2-hydrobenzo ldlthiazol-2-yemethylene) 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-chlorophenyebenzoldlthiazol-3(2H)-yethiaol-2-yl)-N-(4-substituted phenylimino)-3-substituted-2-hydrobenzo thiazole-2-carboxamidine (4a-4h) and (Z)-N'-(4-(2-(4-chlomphenyebenzo [d] thiazol-3(2H)-yl) oxazol-2-yl)-N-(4-substituted phenylimino)-3-substituted-2-hydrobenzo thiazole-2-carboxamidine (4a'-4h') were synthesized starting from 2-chloro-1-(2-(4-chlomphenyebenzoldlthiazol-3(2H)-yl) ethanone (1). The structure configuration of newly synthesized compounds has been determined by elemental analysis and various spectroscopic (IR, (HNMR)-H-1 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-chlomphenyebenzoldlthiazol-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.

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