Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural …

…, ML Hoefle, CD Stratton, DR Sliskovic…

Index: Roth, B. D.; Ortwine, D. F.; Hoefle, M. L.; Stratton, C. D.; Sliskovic, D. R.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 21 - 31

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Citation Number: 56

Abstract

A novel series of trans-6-(2-pyrrol-l-ylethyl)-4-hydroxypyran-2-ones and their dihydroxy acid derivatives were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. A systematic study of substitution at the 2-and 5-positions of the pyrrole ring revealed that optimum potency was realized with the 2-(4-fluorophenyl)-&isopropyl derivative 8x (Table In), which possessed 30% of the in vitro activity of the potent fungal ...