Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold
HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC50 of 3 nM against wild type HIV infected T-cells.
Jones, Eric D.,Vandegraaff, Nick,Le, Giang,Choi, Neil,Issa, William,MacFarlane, Katherine,Thienthong, Neeranat,Winfield, Lisa J.,Coates, Jonathan A.V.,Lu, Long,Li, Xinming,Feng, Xiao,Yu, Changjiang,Rhodes, David I.,Deadman, John J.
