Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.

@article{Fader2014DiscoveryOB,
  title={Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.},
  author={Lee D. Fader and Eric Malenfant and Mathieu Parisien and Rebekah J. Carson and François Bilodeau and Serge Landry and Marc Pesant and C Brochu and S{\'e}bastien Morin and Catherine Chabot and Ted Halmos and Yves Bousquet and Murray D. Bailey and Stephen H. Kawai and R. H. Coulombe and Steven R LaPlante and Araz Jakalian and Punit Kumar Bhardwaj and Dominik Wernic and Patricia Schroeder and Ma'an Amad and Paul Edwards and Michel Garneau and Jianmin Duan and Michael Graham Cordingley and Richard J. Bethell and Stephen W. Mason and Michael Boes and Pierre R. Bonneau and M. Poupart and A. Faucher and Bruno Simoneau and Craig Fenwick and Christiane Yoakim and Youla S Tsantrizos},
  journal={ACS medicinal chemistry letters},
  year={2014},
  volume={5 4},
  pages={
          422-7
        }
}
An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization beginning with compound 1 established the importance of the C3 and C4 substituent to antiviral potency against viruses with different aa124/aa125 variants of IN. The importance of the C7 position on the serum shifted potency was established. Introduction of a quinoline substituent at the C4 position provided a balance of… CONTINUE READING

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