1251462-52-8Relevant articles and documents
Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
Le, Giang,Vandegraaff, Nick,Rhodes, David I.,Jones, Eric D.,Coates, Jonathan A.V.,Lu, Long,Li, Xinming,Yu, Changjiang,Feng, Xiao,Deadman, John J.
scheme or table, p. 5013 - 5018 (2010/10/20)
A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent activities against wild-type virus as well as against the viruses with the mutations Q148H/G140S or N155H/E92Q were reported.