Discovery and evaluation of Ca v 3.2-selective T-type calcium channel blockers.

Authors :: Bezençon O
Remeň L
Richard S
Roch C
Kessler M
Ertel EA
Moon R
Mawet J
Pfeifer T
Capeleto B
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Dec 01; Vol. 27 (23), pp. 5326-5331. Date of Electronic Publication: 2017 Sep 30.
Publication Year :: 2017
Abstract: We identified and characterized a series of pyrrole amides as potent, selective Ca <subscript>v</subscript> 3.2-blockers. This series culminated with the identification of pyrrole amides 13b and 26d, with excellent potencies and/or selectivities toward the Ca <subscript>v</subscript> 3.1- and Ca <subscript>v</subscript> 3.3-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.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)