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

Authors
Lee, YS; Lee, BH; Park, SJ; Kang, SB; Rhim, H; Park, JY; Lee, JH; Jeong, SW; Lee, JY
Issue Date
2004-07-05
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.14, no.13, pp.3379 - 3384
Abstract
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.
Keywords
CALCIUM-CHANNELS; PHARMACOLOGICAL-PROPERTIES; THALAMIC NEURONS; IN-VITRO; CARBODIIMIDE; MIBEFRADIL; INHIBITION; THRESHOLD; ALPHA-1H; CONDUCTANCES; CALCIUM-CHANNELS; PHARMACOLOGICAL-PROPERTIES; THALAMIC NEURONS; IN-VITRO; CARBODIIMIDE; MIBEFRADIL; INHIBITION; THRESHOLD; ALPHA-1H; CONDUCTANCES; 3,4-dihydroquinazolines; T-type calcium channel; blockers; mibefradil
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/137413
DOI
10.1016/j.bmcl.2004.04.090
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KIST Article > 2004
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