Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
- Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers
- 우현민; 이윤석; 노은주; 서선희; 송치만; 정혜진; 배애님; 신계정
- T-type calcium channel; Neuropathic pain
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 21, NO 19, 5910-5915
- 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.
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