A novel class of sodium/calcium exchanger inhibitors: design, synthesis, and structure-activity relationships of 4-phenyl-3-(piperidin-4-yl)-3,4-dihyd...

Basic Information

ID: ALA1149425

Journal: Bioorg Med Chem Lett

Title: A novel class of sodium/calcium exchanger inhibitors: design, synthesis, and structure-activity relationships of 4-phenyl-3-(piperidin-4-yl)-3,4-dihydro-2(1H)-quinazolinone derivatives.

Authors: Hasegawa H, Muraoka M, Matsui K, Kojima A.

Abstract: Design, synthesis, and structure-activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives as sodium/calcium (Na+/Ca2+) exchanger inhibitors are described. In these studies, optimization of the substituents at the 3-position of this series of compounds was carried out and dramatic effects of the substituent on the activities were observed. Based on these SAR studies, a highly potent inhibitor of the Na+/Ca2+ exchanger, which showed single-digit-nanomolar activity, was discovered.

CiteXplore: 16249082

DOI: 10.1016/j.bmcl.2005.10.012

Patent ID: