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Paper | Regular issue | Vol 91, No. 9, 2015, pp.1763-1773
Published online, 24th August, 2015
DOI: 10.3987/COM-15-13290
Synthesis and Antihypertensive α-Blocking Activity Evaluation of Thiazole Derivatives Bearing Pyrazole Moiety

Sobhi M. Gomha,* Khaled Khalil, Hassan Abdel-aziz, and Mohamed Abdalla

*Department of Organic Chemistry, Cairo University, Giza-Haram 12613, Egypt

Abstract

A novel, facile reaction for the synthesis of series of thiazole derivatives has been developed from the reaction of the appropriate thiosemicarbazone derivatives and 2-bromo-1-(5-methyl-1-phenyl-1H-pyrazol-4-yl)ethanone in ethanol under reflux. The structures of the newly synthesized products were established on the basis of spectral data (mass, IR, 1H and 13C NMR) and elemental analyses. The pharmacological screening showed that many of the synthesized compounds exhibit a good antihypertensive α-blocking activity and having low toxicity, as compared to Minoxidil.