883976-56-5Relevant articles and documents
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P′2-ligands
Ghosh, Arun K.,Schiltz, Gary,Perali, Ramu Sridhar,Leshchenko, Sofiya,Kay, Stephanie,Walters, D. Eric,Koh, Yasuhiro,Maeda, Kenji,Mitsuya, Hiroaki
, p. 1869 - 1873 (2007/10/03)
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.