Literature DB >> 18289852

Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.

Stephen Hanessian1, Daniel Simard, Malken Bayrakdarian, Eric Therrien, Ingemar Nilsson, Ola Fjellström.   

Abstract

Guided by available X-ray crystal structure data on the serine protease thrombin, a series of pyridin-2-one derivatives were designed and synthesized having diverse functionality at the P(1) and P(3) sites. Potent in vitro activity against thrombin, with excellent selectivity over trypsin was found for selected analogues.

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Year:  2008        PMID: 18289852     DOI: 10.1016/j.bmcl.2008.01.122

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


  1 in total

1.  Identification of berberine as a direct thrombin inhibitor from traditional Chinese medicine through structural, functional and binding studies.

Authors:  Xing Wang; Yuxin Zhang; Ying Yang; Xia Wu; Hantian Fan; Yanjiang Qiao
Journal:  Sci Rep       Date:  2017-03-09       Impact factor: 4.379

  1 in total

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