Synthesis and biological evaluation of novel T-type Ca2+ channel blockers |
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| Authors: | Jung Hee Kyung Doddareddy Munikumar Reddy Cha Joo Hwan Rhim Hyewhon Cho Yong Seo Koh Hun Yeong Jung Bong Young Pae Ae Nim |
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| Affiliation: | Lifescience Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea. |
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| Abstract: | 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. |
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