ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF NOVEL HETEROCYCLIC SUBSTITUTED THIAZOLE DERIVATIVES
Neeharika Yamsani, Raja Sundararajan
Abstract
A set of new heterocyclic substituted thiazole derivatives were synthesized as powerful analgesic and antiinflammatory agents with minimal ulcer index. Spectroscopic and elemental analyses were employed to confirm the chemical structures of the prepared compounds. Molecular properties, ADME properties, drug-likeness scores, and toxicities of title compounds were predicted using insilico studies. In addition, title compounds were docked against two proteins namely, 3KK6 and 3LN1 using AutoDock 4.2. Tail-flick method and carrageenan-induced foot paw oedema methods were used to screen in vitro analgesic and anti-inflammatory activities of title compounds, respectively. Moreover, the ulcerogenicity of potent compounds of the series was also determined. Most of the novel heterocyclic substituted thiazoles produced, mild-to-good analgesic and anti-inflammatory activity with a low-toreasonable ulcer index. Out of thirteen tested derivatives the most potent compound was found to be 1-(4- chlorophenyl)-4-(2-(4-(4-methoxyphenyl)thiazol-2-yl)hydrazono)-3-methyl-1H-pyrazol-5(4H)-one.