Synthesis and biological evaluation of novel thio-1,4-dihydropyrimidine-5- carboxylate derivatives

Abstract

We have synthesized ten novel isopropyl 2-(4-substituted benzylthio)-6-methyl-4-phenyl-1,4-dihydropyrimidine-5-carboxylate derivatives (5a-j). All the synthesized compounds were characterized by 1H NMR, 13C NMR, IR, MS and elemental analysis data. Newly synthesized compounds were screened for antiinflammatory activity on acetic acid induced writhing in mice and carrageenan induced paw oedema in rats. Compounds (5g) and (5b) showed a potent antiinflammatory activity (100 % at 100 mg/kg b.w) compared to reference standard drug, nimesulide (100% at 50 mg/kg b.w). The other compounds showed good antiinflammatory activity. All the synthesized compounds were also screened for antioxidant activity, among those three compounds were shown good antioxidant activity by using the in vitro method.