| Literature DB >> 17604626 |
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.Entities:
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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