• Bioorg. Med. Chem. Lett. · Oct 2011

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

    • Hyun Min Woo, Yun Suk Lee, Eun Joo Roh, Seon Hee Seo, Chi Man Song, Hye Jin Chung, Ae Nim Pae, and Kye Jung Shin.
    • Life/Health Division, Korea Institute of Science and Technology, 5 Wolsong-gil, Seongbuk-gu, Seoul 136-791, Republic of Korea.
    • Bioorg. Med. Chem. Lett. 2011 Oct 1; 21 (19): 5910-5.

    AbstractTo 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 α(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 μM=61.85-71.99, hERG channel IC(50)=1.57 ± 0.14-4.98 ± 0.36 μM). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia.Copyright © 2011 Elsevier Ltd. All rights reserved.

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