Literature DB >> 17490877

Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.

Martin C Clasby1, Samuel Chackalamannil, Michael Czarniecki, Darío Doller, Keith Eagen, William J Greenlee, Yan Lin, Jayaram R Tagat, Hsingan Tsai, Yan Xia, Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, George Boykow, Madhu Chintala, Yunsheng Hsieh, Andrew T McPhail.   

Abstract

The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhibition of platelet aggregation in a cynomolgus monkey model after oral administration.

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Year:  2007        PMID: 17490877     DOI: 10.1016/j.bmcl.2007.04.061

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


  5 in total

1.  Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.

Authors:  Mariappan V Chelliah; Keith Eagen; Zhuyan Guo; Samuel Chackalamannil; Yan Xia; Hsingan Tsai; William J Greenlee; Ho-Sam Ahn; Stan Kurowski; George Boykow; Yunsheng Hsieh; Madhu Chintala
Journal:  ACS Med Chem Lett       Date:  2014-03-11       Impact factor: 4.345

2.  Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar.

Authors:  Mariappan V Chelliah; Samuel Chackalamannil; Yan Xia; William J Greenlee; Ho-Sam Ahn; Stan Kurowski; George Boykow; Yunsheng Hsieh; Madhu Chintala
Journal:  ACS Med Chem Lett       Date:  2013-12-18       Impact factor: 4.345

3.  A thermal dehydrogenative Diels-Alder reaction of styrenes for the concise synthesis of functionalized naphthalenes.

Authors:  Laura S Kocsis; Erica Benedetti; Kay M Brummond
Journal:  Org Lett       Date:  2012-08-22       Impact factor: 6.005

Review 4.  Protease-activated receptors and prostaglandins in inflammatory lung disease.

Authors:  Terence Peters; Peter J Henry
Journal:  Br J Pharmacol       Date:  2009-10       Impact factor: 8.739

5.  Intramolecular dehydro-Diels-Alder reaction affords selective entry to arylnaphthalene or aryldihydronaphthalene lignans.

Authors:  Laura S Kocsis; Kay M Brummond
Journal:  Org Lett       Date:  2014-07-25       Impact factor: 6.005

  5 in total

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