Synthesis of Novel 8-Hydroxy Quinolin Based 1,3,4-oxadiazoles and S-substituted 1,2,4-triazole Derivatives and Evaluation of their Anti-inflammatory, Analgesic, Ulcerogenic and Anti-Microbial Activities

Mohammad      Mahboob Alam; Mohammad      Shaharyar; Hinna      Hamid; Syed      Nazreen; Saqlain      Haider; Mohammad      Sarwar Alam

doi:10.2174/157340611797928334

Abstract

A series of novel 2-[4-aryl-5-{(quinolin-8-yloxy)methyl}-4H-1,2,4-triazol-3-ylthio]-1-arylethanones (6a-6j) and 8-{(5-aryl-1,3,4-oxadiazol-2-yl)methoxy}quinolines (7a-7d) were synthesized from the corresponding 4-arnyl-1-(2- quinolin-8-yloxy)acetyl) thiosemicarbazides (4a-4d) and hydrazides (3) respectively. The prepared compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities. The anti-inflammatory activities were determined by carrageenan induced rat paw edema method. Compounds 6c, 6d, 6f 6j, 7b and 7e significantly inhibited the rat paw edema depending upon the dose employed. These compounds exhibited insignificant ulceration compared to the standard drug Indomethacin. The compounds were also evaluated for their in vitro antimicrobial activity. Some compounds have shown moderate to good activity whereas compound 7b has shown significant zone of inhibition compared to the standard drug Ampicillin against Gram negative microorganisms.

Keywords: Anti-inflammatory activity,, analgesic, ulcerogenic, animicrobial, 1,3,4-Oxadiazole derivatives, S-substituted phenacyl 1,2,4-, triazole derivatives, thiosemicarbazides, anti-inflammatory, microorganisms