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
Life Sciences Division, Korea Institute of Science and Technology, KIST, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8. doi: 10.1016/j.bmcl.2006.05.031. Epub 2006 Jul 28.
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.
通过一锅法乌吉多组分反应制备了吗啉 -2- 酮 -5- 甲酰胺衍生物，并评估了它们对 T 型和 N 型 Ca(2+) 通道的阻断作用。其中，化合物 5i 具有最高的活性（IC(50)=0.45±0.02 μM），而化合物 5d、5f、5k、5n、5o 和 6m 对 T 型 Ca(2+) 通道也具有较高的活性和选择性。这些新型骨架显示出强效且选择性的 T 型 Ca(2+) 通道阻断活性。
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