2. Academic Validation
  3. Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers

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

Affiliations

  • 1 Actelion Pharmaceuticals Ltd, Drug Discovery and Preclinical Research & Development, Gewerbestrasse 16, CH-4123 Allschwil, Switzerland. Electronic address: dorte.renneberg@actelion.com.
  • 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.

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