2. Academic Validation
  3. Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers

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

  • Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8. doi: 10.1016/j.bmcl.2006.05.031.
Il Whea Ku 1,  Sangwon Cho,  Munikumar Reddy Doddareddy,  Min Seok Jang,  Gyochang Keum,  Jung-Ha Lee,  Bong Young Chung,  Youseung Kim,  Hyewhon Rhim,  Soon Bang Kang
Affiliations

Affiliation

  • 1 Life Sciences Division, Korea Institute of Science and Technology, KIST, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
PMID: 16876404 DOI: 10.1016/j.bmcl.2006.05.031
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.

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