Woo, Hyun Min Lee, Yun Suk Roh, Eun Joo Seo, Seon Hee Song, Chi Man Chung, Hye Jin Pae, Ae Nim Shin, Kye Jung 2024-01-20T16:03:55Z 2024-01-20T16:03:55Z 2021-09-05 2011-10-01 0960-894X https://pubs.kist.re.kr/handle/201004/129905 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 alpha(1G) calcium channel. Among them, several compounds showed good T-type calcium channel inhibitory activity and minimal off-target activity over hERG channel (% inhibition at 10 mu M = 61.85-71.99, hERG channel IC50 = 1.57 +/- 0.14-4.98 +/- 0.36 mu M). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia. (C) 2011 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. CA2+ CHANNELS MIBEFRADIL DISCOVERY Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers Article 10.1016/j.bmcl.2011.07.087 1 Bioorganic & Medicinal Chemistry Letters, v.21, no.19, pp.5910 - 5915 Bioorganic & Medicinal Chemistry Letters 21 19 5910 5915 scie scopus 000294714400054 2-s2.0-80052555689 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CA2+ CHANNELS MIBEFRADIL DISCOVERY T-type calcium channel Neuropathic pain