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Bioorg Med Chem. 2007 Feb 1;15(3):1409-19. Epub 2006 Nov 10.

Lead discovery and optimization of T-type calcium channel blockers.

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1
Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.

Abstract

A series of compounds were designed as T-type calcium channel blocker containing 6 or 5 pharmacophore features from structure-based virtual screening. To optimize the suggested structure, over 130 derivatives were synthesized and their inhibitory activities on T-type calcium channel were assayed using in vitro screening system with alpha1(G) and alpha1(H) clones. For the compounds with higher activities in FDSS assay system, the efficacy was measured by patch-clamp method. Among the library with 5 features, alkaneamide derivatives (7b, 9j, 11b, 11g, 11h) with 4-arylsubstituted piperazine showed better IC(50) values than Mibefradil.

PMID:
17150365
DOI:
10.1016/j.bmc.2006.11.004
[Indexed for MEDLINE]
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