Literature DB >> 17236765

Identification of novel glycine sulfonamide antagonists for the EP1 receptor.

Stephen C McKeown1, Adrian Hall, Richard Blunt, Susan H Brown, Iain P Chessell, Anita Chowdhury, Gerard M P Giblin, Mark P Healy, Matthew R Johnson, Olivier Lorthioir, Anton D Michel, Alan Naylor, Xiao Lewell, Shilina Roman, Stephen P Watson, Wendy J Winchester, Richard J Wilson.   

Abstract

A high-throughput screen targeting the EP(1) receptor identified non-acidic glycine sulfonamide derivative 2a with a pK(i) of 6.2. Analogue synthesis allowed a thorough investigation of the structure-activity relationship (SAR) and led to a 100-fold increase in recombinant potency.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 17236765     DOI: 10.1016/j.bmcl.2006.12.060

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


  2 in total

1.  A summary of seven- and eight-membered ring sultam syntheses via three Michael addition reactions.

Authors:  Ben Niu; Ping Xie; Min Wang; Yanjie Wang; Wannian Zhao; Charles U Pittman; Aihua Zhou
Journal:  Mol Divers       Date:  2015-04-03       Impact factor: 2.943

2.  Nickel-Catalyzed Cross-Coupling of Aryl Halides with Alkyl Halides: Ethyl 4-(4-(4-methylphenylsulfonamido)-phenyl)butanoate.

Authors:  Daniel A Everson; David T George; Daniel J Weix; Jonas F Buergler; John L Wood
Journal:  Organic Synth       Date:  2013
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.