Literature DB >> 14592520

N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.

Paul D Greenspan1, Kirk L Clark, Scott D Cowen, Leslie W McQuire, Ruben A Tommasi, David L Farley, Elizabeth Quadros, David E Coppa, Zengming Du, Zheng Fang, Huanghai Zhou, John Doughty, Karen T Toscano, Andrew M Wigg, Siyuan Zhou.   

Abstract

To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P(2)-P(3) amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhibitors with excellent oral availability.

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Year:  2003        PMID: 14592520     DOI: 10.1016/j.bmcl.2003.08.006

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


  3 in total

1.  Synthesis, spectroscopic and molecular docking studies on new schiff bases, nucleosides and α-aminophosphonate derivatives as antibacterial agents.

Authors:  Saad H Alotaibi; Hamada H Amer
Journal:  Saudi J Biol Sci       Date:  2020-10-16       Impact factor: 4.219

Review 2.  Protease inhibitors and their peptidomimetic derivatives as potential drugs.

Authors:  Georgie Fear; Slavko Komarnytsky; Ilya Raskin
Journal:  Pharmacol Ther       Date:  2006-09-22       Impact factor: 12.310

3.  Strecker-Derived Methodology for Library Synthesis of N-Acylated α-Aminonitriles.

Authors:  Pedro Gonçalves; Anke Peeraer; Yves Adriaenssens; Lara Zonnekein; Philippe Franck; Bert U W Maes; Koen Augustyns; Pieter Van Der Veken
Journal:  ACS Omega       Date:  2021-01-07
  3 in total

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