Literature DB >> 18378447

Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.

Adrian Hall1, Andy Billinton, Susan H Brown, Anita Chowdhury, Gerard M P Giblin, Paul Goldsmith, David N Hurst, Alan Naylor, Sadhana Patel, Tiziana Scoccitti, Pamela J Theobald.   

Abstract

We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.

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Year:  2008        PMID: 18378447     DOI: 10.1016/j.bmcl.2008.03.018

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


  4 in total

1.  Theoretical studies on the mechanism of Pd2+-catalyzed regioselective C-H alkylation of indole with MesICH2CF3OTf.

Authors:  Yao Shi; Hongsheng Ma; Jiaxuan Shao; Chao Deng
Journal:  J Mol Model       Date:  2021-05-04       Impact factor: 1.810

Review 2.  Classification of scaffold-hopping approaches.

Authors:  Hongmao Sun; Gregory Tawa; Anders Wallqvist
Journal:  Drug Discov Today       Date:  2011-10-26       Impact factor: 7.851

3.  Highly substituted 2-amido-furans from Rh(II)-catalyzed cyclopropenations of ynamides.

Authors:  Hongyan Li; Richard P Hsung
Journal:  Org Lett       Date:  2009-10-01       Impact factor: 6.005

4.  Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

Authors:  Muhammad Taha; Fazal Rahim; Aftab Ahmad Khan; El Hassane Anouar; Naveed Ahmed; Syed Adnan Ali Shah; Mohamed Ibrahim; Zainul Amiruddin Zakari
Journal:  Sci Rep       Date:  2020-05-14       Impact factor: 4.379

  4 in total

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