SYNTHESIS AND PHARMACOLOGICAL EVALUATION: ANTIMICROBIAL, ANTI-INFLAMMATORY, ANALGESIC, ULCEROGENIC PROPERTIES OF SEVERAL BIS-HETEROCYCLIC DERIVATIVES

Abstract

In Medicinal chemistry, heterocyclic derivatives contributed the largest classical division of organic chemistry. Thiadiazole compounds have been know many biological activities such as hypoglycemic, anticancer, anti-inflammatory, anti-asthmatic, antihypertensive and etc. On this research, several 1,1-Bis [2-{2-(5-(arylidene)imino-1,3,4-thiadiazol-2-yl) methyl amino}- 1,3,4-thiadiazo-5-yl] cyclopropane 5(a-h) have been synthesized from cyclopropane dicarboxylic acid comprising thiadiazole moieties. All the synthesized compounds have been characterized by elemental (C,H,N) and spectral (I.R., 1H- NMR, Mass) analysis. Furthermore, all synthesized compounds were screened for their antifungal, antimicrobial, anti-inflammatory, analgesic, ulcerogenic and toxic activities. The Compound 5f, 3-chlorophenyl substituted was found the most potent in antimicrobial spectrum against all the used microbes. On the other hand, compound 5g, 4-hydroxy-3-methoxy phenyl substituted was found the most potent in anti-inflammatory, analgesic, and ulcerogenic activities which further evaluated for lesser toxicity test.

Keywords

• Bis-phenylarylidinylthiadiazolidinone cyclopropane
• anti-microbial
• anti-inflammatory
• analgesic