103521-70-6Relevant articles and documents
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines
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)
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.