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ISSN 2063-5346
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SYNTHESIS AND EVALUATION OF NEWER BENZOTHIAZOLE DERIVATIVES FOR DEVELOPING THE NEW ANALGESIC AND ANTIINFLAMMATORY AGENTS

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Preeti Kumari , Smriti Gohri , Dr. Rustam Ekbbal
» doi: 10.31838/ecb/2023.12.s3.755

Abstract

This investigation is divided into two parts: synthesis and biological evaluation. The aim was to synthesize benzothiazole 1, 3, 4-oxadiazole derivatives based on their potential antiinflammatory and analgesic activities. Two series of compounds were prepared: 2-(5- substituted-1, 3, 4-oxadiazole-2-yl)-1, 3-benzothiazole and N-(2, 3-dimethylphenyl)-2-(5- substituted-1, 3, 4-oxadiazole-2-yl) benzenamine. The synthesized compounds were characterized using advanced analytical techniques such as FTIR spectroscopy, hydrogen-1 NMR, and mass spectroscopy. The biological evaluation of the synthesized compounds was performed using Carrageenan-induced acute paw edema in rats and Eddy's hot plate method to assess their anti-inflammatory and analgesic activities, respectively. Screening at the initial level was conducted for each compound, followed by further evaluation using in-vivo models. Compound Vt8 from Scheme 1 exhibited equipotent anti-inflammatory efficacy compared to the standard drug Diclofenac sodium. Compound Vt-9 to Vt-14 showed moderate antiinflammatory efficacy. In analgesic screening, compound Vt11 displayed equipotent activity compared to the standard drug pentazocine. Several other compounds from both series showed excellent or moderate analgesic efficacy. The study concluded that the presence of specific substitutions in the 1, 3, 4-oxadiazole ring led to enhanced anti-inflammatory and analgesic activities. The findings supported the need for further derivatization of the synthesized compounds to explore structure-activity relationships. The research aligns with previous studies on synthetic patterns of 1, 3, 4-oxadiazole analogues and their antiinflammatory and analgesic properties. The results suggest that more 1, 3, 4-oxadiazole analogues can be synthesized by substituting other positions of benzothiazole/1, 3, 4- oxadiazole to develop potent biological agents. The highly potent compounds identified in this study warrant further investigation for their analgesic and anti-inflammatory potential. Future research should focus on elucidating the molecular mechanisms of 1, 3, 4-oxadiazole analogues and conducting clinical studies to develop new analgesic and anti-inflammatory drugs with reduced side effects.

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