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. (C) 2010 Elsevier Ltd. All rights reserved.