Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines
A number of known 1,4-dihydropyridine CCBs were identified as having comparable potency to the steroidal MR antagonist eplerenone. Chiral resolution of mebudipine revealed that MR and CCB activity reside in opposite enantiomers. Small molecule X-ray crystal structures showed that the C4 stereochemistry of optimized selective MR analogues, e.g. 5, is consistent with MR-active mebudipine. Molecular modeling supports a binding pose consistent with that previously proposed for DHP diesters.
Arhancet, Graciela B.,Woodard, Scott S.,Dietz, Jessica D.,Garland, Danny J.,Wagner, Grace M.,Iyanar, Kaliappan,Collins, Joe T.,Blinn, James R.,Numann, Randal E.,Hu, Xiao,Huang, Horng-Chih
supporting information; experimental part
p. 4300 - 4304
(2010/08/22)
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