115672-63-4Relevant academic research and scientific papers
Inhibitors of Cholesterol Biosynthesis. 3. Tetrahydro-4-hydroxy-6--2H-pyran-2-one Inhibitors of HMG-CoA Reductase. 2. Effects of Introducing Substituents at Positions Three and Four of the Pyrrole Nucleus
Roth, B. D.,Blankley, C. J.,Chucholowski, A. W.,Ferguson, E.,Hoefle, M. L.,et al.
, p. 357 - 366 (2007/10/02)
A series of trans-tetrahydro-4-hydroxy-6--2H-pyran-2 ones and their dihydroxy acids were prepared and tested for their ability to inhibit the enzyme HMG-CoA reductase in vitro.Inhibitory potency was found to increase subtantially when substituents were introduced into positions three and four of the pyrrole ring.A systematic exploration of structure-activity relationships at these two positions led to the identification of a compound ((+)-33, (+)-(4R)-trans-2-(4-fluorophenyl)-5-(1-methylethyl)-N,3-diphenyl-1- -1H-pyrrole-4-carboxamide) with five times the inhibitory potency of the fungal metabolite compactin.
TRANS-6-[2-[2-(SUBSTITUTED-PHENYL)-3- (OR 4-) HETEROARYL-5-SUBSTITUTED-1H-PYRROL-1-YL]-ETHYL]TETRAHYDRO-4-HYDROXY-2H-PYRAN-2-ONE INHIBITORS OF CHOLESTEROL BIOSYNTHESIS
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, (2008/06/13)
Certain trans-6-2-2-(substituted-phenyl)-3-(or 4-) heteroaryl-5-substituted-1H-pyrrol-1-yl!ethyl!tetrahydro-4-hydroxy-2H-py ran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme
