Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers

  • Bioorg Med Chem Lett. 2015 Sep 15;25(18):3941-6. doi: 10.1016/j.bmcl.2015.07.038.
Dorte Renneberg  1 ,  Francis Hubler  2 ,  Markus Rey  2 ,  Patrick Hess  2 ,  Stephane Delahaye  2 ,  John Gatfield  2 ,  Marc Iglarz  2 ,  Kurt Hilpert  2
Affiliations
  • 1. Actelion Pharmaceuticals Ltd, Drug Discovery and Preclinical Research & Development, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland. Electronic address: [email protected].
  • 2. Actelion Pharmaceuticals Ltd, Drug Discovery and Preclinical Research & Development, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland.
PMID: 26231163 DOI: 10.1016/j.bmcl.2015.07.038
Abstract

Chemical evolution of mibefradil resulted in the identification of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. A SAR study, in vitro and in vivo DMPK properties as well as the in vivo antihypertensive effect in rats are presented.

Keywords
Antihypertensive effect; Bridged tetrahydronaphthalene; Calcium channel blocker; Mibefradil; T/L-type calcium channels.