Literature DB >> 16876404

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

Il Whea Ku1, Sangwon Cho, Munikumar Reddy Doddareddy, Min Seok Jang, Gyochang Keum, Jung-Ha Lee, Bong Young Chung, Youseung Kim, Hyewhon Rhim, Soon Bang Kang.   

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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Year:  2006        PMID: 16876404     DOI: 10.1016/j.bmcl.2006.05.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

2.  One-pot multicomponent synthesis of two novel thiolactone scaffolds.

Authors:  B Beck; S Srivastava; K Khoury; E Herdtweck; Alexander Dömling
Journal:  Mol Divers       Date:  2010-04-21       Impact factor: 2.943

3.  Efficient assembly of iminodicarboxamides by a "truly" four-component reaction.

Authors:  Kareem Khoury; Mantosh K Sinha; Tadamichi Nagashima; Eberhardt Herdtweck; Alexander Dömling
Journal:  Angew Chem Int Ed Engl       Date:  2012-09-11       Impact factor: 15.336

  3 in total

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