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. 1986 May;29(5):849-52.
doi: 10.1021/jm00155a040.

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin

W F Hoffman, A W Alberts, P S Anderson, J S Chen, R L Smith, A K Willard

3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin

W F Hoffman et al. J Med Chem. 1986 May.

Abstract

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 alpha to the carbonyl group increased potency. This observation led to the synthesis of compound 16, which has about 2.5 times the intrinsic inhibitory activity of mevinolin.

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