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

@article{Jones2010DesignOA,
  title={Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.},
  author={Eric Dale Jones and Nick Vandegraaff and Giang Thi Truc Le and Neil Choi and William Issa and Katherine J Macfarlane and Neeranat Thienthong and Lisa J Winfield and Jonathan Alan Victor Coates and Long Lu and Xinming Li and Xiao Ling Feng and Changjiang Yu and David Ian Rhodes and John J. Deadman},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 19},
  pages={5913-7}
}
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. 

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