Literature DB >> 12749892

N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.

George A Doherty1, Ginger X Yang, Edite Borges, Sharon Tong, Ermengilda D McCauley, Kelly M Treonz, Gail Van Riper, Stephen Pacholok, Qian Si, Gloria C Koo, Kashmira Shah, Richard A Mumford, William K Hagmann.   

Abstract

A series of isonicotinoyl-(L)-aminophenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. These compounds exhibit subnanomolar binding affinity to VLA-4 and significant off-rates. The interplay between off-rate, protein binding and pharmacokinetics is discussed.

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Year:  2003        PMID: 12749892     DOI: 10.1016/s0960-894x(03)00308-1

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


  2 in total

1.  Exploring N-Arylsulfonyl-l-proline Scaffold as a Platform for Potent and Selective αvβ1 Integrin Inhibitors.

Authors:  Nilgun Isik Reed; You-Zhi Tang; Joel McIntosh; Yibing Wu; Kathleen S Molnar; Annafelicia Civitavecchia; Dean Sheppard; William F DeGrado; Hyunil Jo
Journal:  ACS Med Chem Lett       Date:  2016-08-30       Impact factor: 4.345

2.  Stereoselective Synthesis of Quaternary Proline Analogues.

Authors:  M Isabel Calaza; Carlos Cativiela
Journal:  European J Org Chem       Date:  2008
  2 in total

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