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Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers


Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers



Bioorganic and Medicinal Chemistry Letters 15(2): 283-286



ISSN/ISBN: 0960-894X

PMID: 15603940

DOI: 10.1002/chin.200520151

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca2+ channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca2+ channels and N-type Ca2+ channels. Among them, 5b (KYS05044, IC50 = 0.56 +/- 0.10 muM) was identified as potent T-type Ca2+ channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI = >100). Copyright 2004 Elsevier Ltd.

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Accession: 012609986

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