Literature DB >> 17604626

Benzyl amide-ketoacid inhibitors of HIV-integrase.

Michael A Walker1, Timothy Johnson, B Narasimhulu Naidu, Jacques Banville, Roger Remillard, Serge Plamondon, Alain Martel, Chen Li, Albert Torri, Himadri Samanta, Zeyu Lin, Ira Dicker, Mark Krystal, Nicholas A Meanwell.   

Abstract

Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. Previous reports have demonstrated that the diketoacid-based chemotype is a useful starting point for the design of inhibitors of this enzyme. In this study, one of the ketone groups is replaced by a benzylamide resulting in a new potent chemotype. A preliminary SAR study is carried out to investigate the substitution requirements on the phenyl ring and methylene group of the benzylamide.

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Year:  2007        PMID: 17604626     DOI: 10.1016/j.bmcl.2007.06.042

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


  3 in total

Review 1.  Authentic HIV-1 integrase inhibitors.

Authors:  Chenzhong Liao; Christophe Marchand; Terrence R Burke; Yves Pommier; Marc C Nicklaus
Journal:  Future Med Chem       Date:  2010-07       Impact factor: 3.808

2.  Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones.

Authors:  Xue Zhi Zhao; Kasthuraiah Maddali; B Christie Vu; Christophe Marchand; Stephen H Hughes; Yves Pommier; Terrence R Burke
Journal:  Bioorg Med Chem Lett       Date:  2009-03-28       Impact factor: 2.823

3.  Diketoacid-genre HIV-1 integrase inhibitors containing enantiomeric arylamide functionality.

Authors:  Xue Zhi Zhao; Kasthuraiah Maddali; Christophe Marchand; Yves Pommier; Terrence R Burke
Journal:  Bioorg Med Chem       Date:  2009-05-08       Impact factor: 3.641

  3 in total

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