0 citations
Stereochemical Requirements for the Mineralocorticoid Receptor Antagonist Activity of Dihydropyridines
Journal of Medicinal Chemistry2010Vol. 53(10), pp. 4300–4304
Citations Over TimeTop 10% of 2010 papers
Graciela B. Arhancet, Scott S. Woodard, Jessica D. Dietz, Danny J. Garland, Grace M. Wagner, Kaliappan Iyanar, Joe Collins, James R. Blinn, Randal Numann, Xiao Hu, H. T. 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.
Related Papers
- → Mineralocorticoid Receptor Blockade in the Protection of Target Organ Damage(2006)45 cited
- → Molecular Mechanisms of Mineralocorticoid Receptor Antagonism by Eplerenone(2005)38 cited
- → Interactions of High Salt Intake and the Response of the Cardiovascular System to Aldosterone(2005)17 cited
- → Minelarocorticoid Receptor is Overexpressed in Cardiomyocytes of Patients with Congestive Heart Failure(2012)