Synthesis and biological activity of methanesulfonamide pyrimidine-and N-methanesulfonyl pyrrole-substituted 3, 5-dihydroxy-6-heptenoates, a novel series of HMG- …

M Watanabe, H Koike, T Ishiba, T Okada, S Seo…

Index: Watanabe, Masamichi; Koike, Haruo; Ishiba, Teruyuki; Okada, Tetsuo; Seo, Shujiro; Hirai, Kentaro Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 2 p. 437 - 444

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Citation Number: 126

Abstract

A novel series of methanesulfonamide pyrimidine-and N-methanesulfonyl pyrrole- substituted 3, 5-dihydroxy-6-heptenoates were synthesized and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. Monocalcium bis (+)-7-[4-(4-fluorophenyl)-6- isopropyl-2-(N-methyl-N-methanesulfonylaminopyrimidin)-5-yl]-(3R, 5S)-dihydroxy-(E)-6- heptenoate (3a, S-4522) was selected as a candidate for further evaluation. Compound ...