Literature DB >> 15261262

Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.

Matthew M Morrissette1, Kenneth J Stauffer, Peter D Williams, Terry A Lyle, Joseph P Vacca, Julie A Krueger, S Dale Lewis, Bobby J Lucas, Bradley K Wong, Rebecca B White, Cynthia Miller-Stein, Elizabeth A Lyle, Audrey A Wallace, Yvonne M Leonard, Denise C Welsh, Joseph J Lynch, Daniel R McMasters.   

Abstract

Modification of lead compound 1 by reducing lipophilicity in the P3 group produced a series of low molecular weight thrombin inhibitors with excellent potency in functional assays, metabolic stability, and oral bioavailability. These modifications led to the identification of two optimized compounds, 14 and 16.

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Year:  2004        PMID: 15261262     DOI: 10.1016/j.bmcl.2004.06.030

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


  1 in total

1.  Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.

Authors:  Harry R Chobanian; Barbara Pio; Yan Guo; Hong Shen; Mark A Huffman; Maria Madeira; Gino Salituro; Jenna L Terebetski; James Ormes; Nina Jochnowitz; Lizbeth Hoos; Yuchen Zhou; Dale Lewis; Brian Hawes; Lyndon Mitnaul; Kim O'Neill; Kenneth Ellsworth; Liangsu Wang; Tesfaye Biftu; Joseph L Duffy
Journal:  ACS Med Chem Lett       Date:  2015-03-13       Impact factor: 4.345

  1 in total

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