Synthesis and SAR studies of a novel series of T-type calcium channel blockers

Park, SJ; Park, SJ; Lee, MJ; Rhim, H; Kim, Y; Lee, JH; Chung, BY; Lee, JY

doi:10.1016/j.bmc.2006.01.005

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Synthesis and SAR studies of a novel series of T-type calcium channel blockers

Park, SJ;
Park, SJ;
Lee, MJ;
Rhim, H;
Kim, Y;
... Lee, JH;
외 2명

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WEB OF SCIENCE

33

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SCOPUS

34

초록

For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among them, 9c (KYS05064, IC50 = 0.96 +/- 0.22 mu M) was found to be as potent as Mibefradil and also showed the highest selectivity for T-type Ca2+ channel with no effect on N-type Ca2+ channel. (c) 2006 Published by Elsevier Ltd.

키워드

T-type calcium channel blockers; selectivity; potency; 3,4-dihydroquinazoline; sulfonamido group; IN-VITRO; INHIBITION; NEURONS; CLONING; MEMBER

제목: Synthesis and SAR studies of a novel series of T-type calcium channel blockers

저자: Park, SJ; Park, SJ; Lee, MJ; Rhim, H; Kim, Y; Lee, JH; Chung, BY; Lee, JY

DOI: 10.1016/j.bmc.2006.01.005

발행일: 2006-05-15

유형: Article

저널명: Bioorganic and Medicinal Chemistry

권: 14

호: 10

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