Synthesis and in vitro screening of some 1,3,4-oxadiazole derivatives as lipoxygenase inhibitors

eng Oriental Scientific Publishing Company Biosciences Biotechnology Research Asia 0973-1245 2016-02-03 4 2 609 614 6010 article Synthesis and in vitro screening of some 1,3,4-oxadiazole derivatives as lipoxygenase inhibitors P.Y. Pawar 1 S.G. Kaskhedikar 2 Department of Pharmchemistry, P.D.V.V.P.F’s College of Pharmacy, Vilad Ghat, Ahmednagar - 414 111, (India). Department of Pharmacy, S.G.S.I.TS., 23 Park Road, Vallabhnagar, Indore - 03, (India). 1,3,4-oxadiazole derivatives of some classical Non Steroidal Anti-inflammatory Drugs were synthesized and investigated for the lipoxygenase inhibitory activity in vitro. The target compounds were obtained by cyclodesulfurization of the corresponding thiosemicarbazides using I2/NaOH. The intermediates were readily accessible through conversion of the carboxylic acid group to the respective acid hydrazides followed by treatment with phenyl isothiocyanate to yield corresponding thiosemicarbazides. The constitution of the products was confirmed by spectroscopic and elemental analysis. All the synthesized oxadiazole derivatives exhibited significant lipoxygenase inhibitory activity. https://www.biotech-asia.org/vol4no2/synthesis-and-in-vitro-screening-of-some-134-oxadiazole-derivatives-as-lipoxygenase-inhibitors/ 1 3 4-oxadiazole; Lipoxygenase inhibition; NSAIDs