| Literature DB >> 20408553 |
Graciela B Arhancet1, Scott S Woodard, Jessica D Dietz, Danny J Garland, Grace M Wagner, Kaliappan Iyanar, Joe T Collins, James R Blinn, Randal E Numann, Xiao Hu, Horng-Chih Huang.
Abstract
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.Entities:
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Year: 2010 PMID： 20408553 DOI： 10.1021/jm1002827
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446