HMG-CoA reductase inhibitors: Design, synthesis, and biological activity of tetrahydroindazole-substituted 3, 5-dihydroxy-6-heptenoic acid sodium salts

PJ Connolly, CD Westin, DA Loughney…

Index: Connolly, Peter J.; Westin, Claudia D.; Loughney, Deborah A.; Minor, Lisa K. Journal of Medicinal Chemistry, 1993 , vol. 36, # 23 p. 3674 - 3685

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Citation Number: 30

Abstract

Compounds comprising a series of 7-[2-(4-fluorophenyl)-4, 5, 6, 7-tetrahydr~~-ind~ ol-3-y1]- 3, 5-dihydroxy-6-heptenoic acid sodium salts (18) were synthesized and tested for their ability to inhibit HMG-CoA reductase in a partially purified enzyme preparation and cholesterol biosynthesis from acetate in cultured HEP-GO cells. Changing the size of the saturated ring of the tetrahydroindazole nucleus did not improve potency, but ...