Title of article :
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the -ligands
Author/Authors :
Arun K. Ghosh، نويسنده , , Gary Schiltz، نويسنده , , Ramu Sridhar Perali، نويسنده , , Sofiya Leshchenko، نويسنده , , Stephanie Kay، نويسنده , , D. Eric Walters، نويسنده , , Yasuhiro Koh، نويسنده , , Kenji Maeda، نويسنده , , Hiroaki Mitsuya، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
Abstract :
A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 2 (TMC-114) bound to HIV-1 protease. The effects of substituents, spirocyclic rings, and ring sizes have been investigated. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV protease.
Keywords :
HIV proptease , Oxyindole , TMC-114 , design , synthesis , inhibitors
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
