Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers

…, YS Lee, EJ Roh, SH Seo, CM Song, HJ Chung…

Index: Woo, Hyun Min; Lee, Yun Suk; Roh, Eun Joo; Seo, Seon Hee; Song, Chi Man; Chung, Hye Jin; Pae, Ae Nim; Shin, Kye Jung Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5910 - 5915

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Citation Number: 7

Abstract

To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 4-piperidinecarboxylate and 4-piperidinecyanide derivatives were prepared and evaluated for in vitro and in vivo activity against α1G calcium channel. Among them, several compounds showed good T-type calcium channel inhibitory activity and minimal off-target activity over hERG channel (% inhibition at 10μM= 61.85–71.99, hERG channel IC50= ...