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Morpholin-2-one derivatives as novel selective T-type Ca<SUP>2+</SUP> channel blockers
- Ku, Il Whea;
- Cho, Sangwon;
- Doddareddy, Munikumar Reddy;
- Jang, Min Seok;
- Keum, Gyochang;
- ... Lee, Jung-Ha;
- 외 4명
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41초록
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.
키워드
T-type Ca2+ channel; mibefradil; morpholinone; CALCIUM-CHANNELS; EFFICIENT SYNTHESIS; IN-VITRO; NEURONS; PAIN; DIVERSITY; SUBUNITS; EPILEPSY; RECEPTOR
- 제목
- Morpholin-2-one derivatives as novel selective T-type Ca<SUP>2+</SUP> channel blockers
- 저자
- 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
- 발행일
- 2006-10-01
- 유형
- Article
- 권
- 16
- 호
- 19
- 페이지
- 5244 ~ 5248