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 2024-01-21T02:05:29Z 2024-01-21T02:05:29Z 2021-09-01 2006-10-01 0960-894X https://pubs.kist.re.kr/handle/201004/135036 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 mu M), 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. (c) 2006 Published by Elsevier Ltd. English PERGAMON-ELSEVIER SCIENCE LTD CALCIUM-CHANNELS EFFICIENT SYNTHESIS IN-VITRO NEURONS PAIN DIVERSITY SUBUNITS EPILEPSY RECEPTOR Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers Article 10.1016/j.bmcl.2006.05.031 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.16, no.19, pp.5244 - 5248 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 16 19 5244 5248 scie scopus 000240615400051 2-s2.0-33747330904 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CALCIUM-CHANNELS EFFICIENT SYNTHESIS IN-VITRO NEURONS PAIN DIVERSITY SUBUNITS EPILEPSY RECEPTOR T-type Ca2+ channel mibefradil morpholinone