Author/Authors :
Il Whea Ku، نويسنده , , Sangwon Cho، نويسنده , , Munikumar Reddy Doddareddy، نويسنده , , Min Seok Jang، نويسنده , , Gyochang Keum، نويسنده , , Jung-Ha Lee، نويسنده , , Bong Young Chung، نويسنده , , Youseung Kim، نويسنده , , Hyewhon Rhim، نويسنده , , Soon Bang Kang، نويسنده ,
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 Ca2+ channels. Among them, compound 5i produced the highest potency (IC50 = 0.45 ± 0.02 μM), while compounds 5d, 5f, 5k, 5n, 5o, and 6m produced relatively high potency as well as selectivity on T-type Ca2+ channels. These novel scaffolds showed potent and selective T-type Ca2+ channel blocking activities.
