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Discovery and evaluation of Cav3.2-selective T-type calcium channel blockers
Authors:Olivier Bezençon  Lubo? Remeň  Sylvia Richard  Catherine Roch  Melanie Kessler  Eric A Ertel  Richard Moon  Jacques Mawet  Thomas Pfeifer  Bruno Capeleto
Institution:Drug Discovery Chemistry, Biology and Pharmacology, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, CH-4123 Allschwil, Switzerland
Abstract:We identified and characterized a series of pyrrole amides as potent, selective Cav3.2-blockers. This series culminated with the identification of pyrrole amides 13b and 26d, with excellent potencies and/or selectivities toward the Cav3.1- and Cav3.3-channels. These compounds display poor physicochemical and DMPK properties, making their use difficult for in vivo applications. Nevertheless, they are well-suited for in vitro studies.
Keywords:AcOH  acetic acid  Boc  DIPEA  DMAP  4-(dimethylamino)pyridine  DMF  EDC·HCl  1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride  HOBt  hydroxybenzotriazole  KHMDS  potassium hexamethyldisilylazide  Ms  mesyl(methylsulfonyl)  NBS  NCS  Tf  trifluorosulfonyl  THF  tetrahydrofuran  T-type calcium channel  Selective Cav3  2-blockers  Pyrroles  Absence-type epilepsy
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