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

Title
Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
Authors
우현민이윤석노은주서선희송치만정혜진배애님신계정
Keywords
T-type calcium channel; Neuropathic pain
Issue Date
2011-10
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 21, NO 19, 5910-5915
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 a1G 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 IC50 = 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.
URI
http://pubs.kist.re.kr/handle/201004/45639
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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