Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers |
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| Authors: | Ku Il Whea Cho Sangwon Doddareddy Munikumar Reddy Jang Min Seok Keum Gyochang Lee Jung-Ha Chung Bong Young Kim Youseung Rhim Hyewhon Kang Soon Bang |
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| Institution: | Life Sciences Division, Korea Institute of Science and Technology, KIST, PO Box 131, Cheongryang, Seoul 130-650, South Korea. |
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| Abstract: | Morpholin-2-one-5-carboxamide derivatives were prepared by using the one-pot Ugi multicomponent reaction and evaluated for blocking effects on T- and N-type Ca(2+) channels. Among them, compound 5i produced the highest potency (IC(50)=0.45+/-0.02 microM), while compounds 5d, 5f, 5k, 5n, 5o, and 6m produced relatively high potency as well as selectivity on T-type Ca(2+) channels. These novel scaffolds showed potent and selective T-type Ca(2+) channel blocking activities. |
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