3-Hydroxy-3-methylglutaryl-coenzyme A Reductase Inhibitors. 4. Side Chain Ester Derivatives of Mevinolin

Article abstract of DOI:10.1021/jm00155a040

Modification of the 2(S)-methylbutyryl moiety of mevinolin led to a series of side chain ester derivatives.A systematic exploration of the structure-activity relationships showed that the introduction of an additional aliphatic group on the carbon α to the carbonyl group increased potency.This obsrevation led to the synthesis of compound 16, which has about 2.5 times the intrinsic inhibitory activity of mevinolin.