Journal of Medicinal Chemistry p. 849 - 852 (1986)
Update date:2022-08-03
Topics:
Hoffman, W. F.
Alberts, A. W.
Anderson, P. S.
Chen, J. S.
Smith, R. L.
Willard, A. K.
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.
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