Studies on Hypolipidemic Agents. IV.1) Syntheses and Biological Activities of trans- and cis-2-(4-Alkylcyclohexyl)- Arenesulfonates

Abstract

trans- and cis-2-Diazo-1-(4-alkylcyclohexyl)-1-ethanones were reacted with arenesulfonic acids to afford the corresponding 2-(4-alkylcyclohexyl)-2-oxoethyl arenesulfonates. The esterase-inhibitory activity and hypolipidemic effect of the arenesulfonates were examined, and it was found that in most cases, the trans-isomers were more active than the corresponding cis-isomers. Stereoselective syntheses of several biologically potent trans-isomers ( trans-3) were also developed. © 1987, The Pharmaceutical Society of Japan. All rights reserved.