Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold

  • Bioorg Med Chem Lett. 2010 Oct 1;20(19):5913-7. doi: 10.1016/j.bmcl.2010.07.079.
Eric D Jones  1 ,  Nick Vandegraaff ,  Giang Le ,  Neil Choi ,  William Issa ,  Katherine Macfarlane ,  Neeranat Thienthong ,  Lisa J Winfield ,  Jonathan A V Coates ,  Long Lu ,  Xinming Li ,  Xiao Feng ,  Changjiang Yu ,  David I Rhodes ,  John J Deadman
Affiliations
  • 1. Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia.
PMID: 20727748 DOI: 10.1016/j.bmcl.2010.07.079
Abstract

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 EC(50) of 3 nM against wild type HIV infected T-cells.