Author/Authors :
Michael A. Walker، نويسنده , , Timothy Johnson، نويسنده , , B. Narasimhulu Naidu، نويسنده , , Jacques Banville، نويسنده , , Roger Remillard، نويسنده , , Serge Plamondon، نويسنده , , Alain Martel، نويسنده , , Chen Li، نويسنده , , Albert Torri، نويسنده , , Himadri Samanta، نويسنده , , Zeyu Lin، نويسنده , , Ira Dicker، نويسنده , , Mark Krystal، نويسنده , , Nicholas A. Meanwell، نويسنده ,
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.
Keywords :
HIV , antiviral , AIDS , Diketoacid , Amide-ketoacid , integrase
