Synthesis and pharmacological evaluation of 5-methyl-2-phenylthiazole-4-substituted heteroazoles as a potential anti-inflammatory and analgesic agents

AbstractA series of novel 5-methyl-2-phenylthiazole-4-substituted-heteroazole derivatives (6–15) have been synthesized. The structures of these compounds were established by IR, 1HNMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activities as well as gastric ulcerogenic effects. Derivatives 9, 10, 14 and 15 exhibited moderate to good anti-inflammatory and analgesic activities in carrageenan-induced rat paw edema and acetic acid-induced writhing in mice respectively, with low ulcerogenicity compared with the standard drug diclofenac sodium

Novel ethyl-5-amino-3-methylthio-1H-pyrazole-4-carboxylates: Synthesis and pharmacological activity

A series of novel ethyl-5-amino-3-methylthio-1H-pyrazole-4-carboxylates 3a–j were synthesized from condensation of various hydrazides 2a–j with ketene dithioacetal. The synthesized compounds were screened for in vivo analgesic and anti-inflammatory activities using acetic acid writhing test in mice and carrageenan-induced paw edema test in rat, respectively. Diclofenac sodium was used as a standard drug for comparison. Compounds 3a, 3c and 3d exhibited significant analgesic and anti-inflammatory activities at a dose of 25 mg/kg and showed quite less ulcerogenic index in the range of 0.9–1.12 whereas diclofenac sodium showed 3.10