Literature DB >> 16263291

Design, synthesis, and biological activity of novel factor Xa inhibitors: improving metabolic stability by S1 and S4 ligand modification.

Satoshi Komoriya1, Shozo Kobayashi, Ken Osanai, Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Yumi Nakamoto, Akiyoshi Mochizuki, Takayasu Nagahara, Makoto Suzuki, Takashi Shimada, Kengo Watanabe, Yumiko Isobe, Taketoshi Furugoori.   

Abstract

Serine protease factor xa (fXa) inhibitor 1 showed good ex vivo anti-fXa activity upon oral administration in rats. However, it has been revealed that 1 had low metabolic stability against human liver microsomes. To improve the metabolic stability, we attempted to modify the S1 and S4 ligands of 1. These modifications resulted in compound 34b, which exhibited selective anti-fXa activity and excellent anti-coagulation activity.

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Year:  2005        PMID： 16263291     DOI： 10.1016/j.bmc.2005.09.056

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  3 in total

1.  A lead discovery strategy driven by a comprehensive analysis of proteases in the peptide substrate space.

Authors:  Sai Chetan K Sukuru; Florian Nigsch; Jean Quancard; Martin Renatus; Rajiv Chopra; Natasja Brooijmans; Dmitri Mikhailov; Zhan Deng; Allen Cornett; Jeremy L Jenkins; Ulrich Hommel; John W Davies; Meir Glick
Journal:  Protein Sci       Date:  2010-11       Impact factor: 6.725

2.  A novel and expedient approach to new thiazoles, thiazolo[3,2-a]pyridines, dihydrothiophenes, and hydrazones incorporating thieno[2,3-b]thiophene moiety.

Authors:  Yahia Nasser Mabkhot; Assem Barakat; Abdullah Mohammad Al-Majid; Abdullah Saleh Alamary; Taleb T Al-Nahary
Journal:  Int J Mol Sci       Date:  2012-04-23       Impact factor: 6.208

3.  Mechanistic Insights into Biological Activities of Polyphenolic Compounds from Rosemary Obtained by Inverse Molecular Docking.

Authors:  Samo Lešnik; Urban Bren
Journal:  Foods       Date:  2021-12-28
  3 in total

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