Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers |
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Authors: | Jie Eun Lee Hun Yeong Koh Seon Hee Seo Yi Yeon Baek Hyewhon Rhim Yong Seo Cho Hyunah Choo Ae Nim Pae |
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Institution: | 1. Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea;2. Department of Chemistry, Inha University, Nam-gu, Incheon 402-751, Republic of Korea |
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Abstract: | T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives substituted with arylpiperazinylalkylamines. The oxazoles were synthesized in a convenient convergent synthetic method, and biologically evaluated against α1G (CaV3.1) T-type calcium channel. Among total 41 oxazole compounds synthesized, the most active one was the compound 10-35 with an IC50 value of 0.65 μM, which is comparable with that of mibefradil. |
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