Morpholin-2-one derivatives as novel selective T-type Ca super(2+) channel blockers

Morpholin-2-one derivatives as novel selective T-type Ca super(2+) channel blockers

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 super(2+) channels. Among them, compound 5i produced the highest potency (IC sub(50) = 0.45 +/- 0.02 mu M), while compounds 5d, 5f, 5k, 5n,...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (19), p.5244-5248
Hauptverfasser: 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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Sprache:eng
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Zusammenfassung: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 super(2+) channels. Among them, compound 5i produced the highest potency (IC sub(50) = 0.45 +/- 0.02 mu M), while compounds 5d, 5f, 5k, 5n, 5o, and 6m produced relatively high potency as well as selectivity on T-type Ca super(2+) channels. These novel scaffolds showed potent and selective T-type Ca super(2+) channel blocking activities.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.05.031