3,4-dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

Lee, YS; Lee, BH; Park, SJ; Kang, SB; Rhim, H; Park, JY; Lee, JH; Jeong, SW; Lee, JY

doi:10.1016/j.bmcl.2004.04.090

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3,4-dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

Lee, YS;
Lee, BH;
Park, SJ;
Kang, SB;
Rhim, H;
... Lee, JH;
외 3명

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WEB OF SCIENCE

53

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SCOPUS

55

초록

For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS05001, IC50 = 0-9 muM) was nearly equipotent with mibefradil (IC50 = 0.84 muM) and inhibited LVA T-type Ca2+ channel with greater efficacy than HVA Ca2+ channel. (C) 2004 Elsevier Ltd. All rights reserved.

키워드

3,4-dihydroquinazolines; T-type calcium channel; blockers; mibefradil; CALCIUM-CHANNELS; PHARMACOLOGICAL-PROPERTIES; THALAMIC NEURONS; IN-VITRO; CARBODIIMIDE; MIBEFRADIL; INHIBITION; THRESHOLD; ALPHA-1H; CONDUCTANCES

제목: 3,4-dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

저자: Lee, YS; Lee, BH; Park, SJ; Kang, SB; Rhim, H; Park, JY; Lee, JH; Jeong, SW; Lee, JY

DOI: 10.1016/j.bmcl.2004.04.090

발행일: 2004-07-05

유형: Article

저널명: Bioorganic and Medicinal Chemistry Letters

권: 14

호: 13

페이지: 3379 ~ 3384

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3,4-dihydroquinazoline derivatives as novel selective T-type Ca<SUP>2+</SUP> channel blockers

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