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1: Bioorg Med Chem. 2004 Aug 1;12(15):3965-70.Click here to read Links

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

Jung HK, Doddareddy MR, Cha JH, Rhim H, Cho YS, Koh HY, Jung BY, Pae AN.

Lifescience Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.

A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca(2+) channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca(2+) channel. The compound 21 with trifluoromethyl substituents at C(3)-position of phenyl group (R(1)) and C(2)-position of phenyl group (R(2)) showed the highest inhibitory activity with IC(50) value of 1.02 microM, which is comparable to that of mibefradil.

PMID: 15246072 [PubMed - indexed for MEDLINE]

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