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Synthesis and biological evaluation of novel T-type Ca2+ channel blockers

Authors
Jung, HK; Doddareddy, MR; Cha, JH; Rhim, H; Cho, YS; Koh, HY; Jung, BY; Pae, AN
Issue Date
2004-08-01
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.12, no.15, pp.3965 - 3970
Abstract
A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca2+ channel. The compound 21 with trifluoromethyl substituents at C-3-position of phenyl group (W) and C-2-position of phenyl group (R-2) showed the highest inhibitory activity with IC50 value of 1.02 muM, which is comparable to that of mibefradil. (C) 2004 Elsevier Ltd. All rights reserved.
Keywords
CALCIUM-CHANNELS; RECEPTOR LIGANDS; CLONED HUMAN; DOPAMINE; ANTAGONIST; INHIBITION; EFFICACY; CURRENTS; AGONIST; DESIGN; CALCIUM-CHANNELS; RECEPTOR LIGANDS; CLONED HUMAN; DOPAMINE; ANTAGONIST; INHIBITION; EFFICACY; CURRENTS; AGONIST; DESIGN; T-type calcium channel; synthesis
ISSN
0968-0896
URI
https://pubs.kist.re.kr/handle/201004/137322
DOI
10.1016/j.bmc.2004.06.011
Appears in Collections:
KIST Article > 2004
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