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ID: ALA1148674

Journal: Bioorg Med Chem Lett

Title: Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers.

Authors: Ku IW, Cho S, Doddareddy MR, Jang MS, Keum G, Lee JH, Chung BY, Kim Y, Rhim H, Kang SB.

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.

CiteXplore: 16876404

DOI: 10.1016/j.bmcl.2006.05.031