912998-81-3Relevant articles and documents
PYRROLE COMPOUNDS AND USES THEREOF
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Page/Page column 51; 52, (2010/11/24)
Pyrrole compounds, compositions and methods are provided for the treatment, prevention, or amelioration of neurodegenerative diseases, cardiovascular diseases, proliferative diseases and visual disorders. In particular, pyrrole compounds, compositions and methods for the treatment of stroke are disclosed herein.
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.