Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5913-7. doi: 10.1016/j.bmcl.2010.07.079. Epub 2010 Jul 27.
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.
呈现了一种基于新型双环嘧啶酮核心的 HIV 整合酶抑制剂。对核心支架的九个变体进行了评估,导致 6:6 核心得到优化,得到化合物 48,对野生型 HIV 感染的 T 细胞的 EC(50)为 3 nM。