Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.

@article{Fenwick2014PreclinicalPO,
  title={Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.},
  author={Craig Fenwick and Ma'an Amad and Murray D. Bailey and Richard J. Bethell and Michael Boes and Pierre R. Bonneau and Michael Graham Cordingley and R. H. Coulombe and Jianmin Duan and Paul Edwards and Lee D. Fader and A. Faucher and Michel Garneau and Araz Jakalian and Stephen H. Kawai and Louie Lamorte and Steven R LaPlante and Laibin Luo and Steve Mason and M. Poupart and Nathalie Rioux and Patricia Schroeder and Bruno Simoneau and Sonia Tremblay and Youla S Tsantrizos and Myriam Witvrouw and Christiane Yoakim},
  journal={Antimicrobial agents and chemotherapy},
  year={2014},
  volume={58 6},
  pages={
          3233-44
        }
}
BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand transfer inhibitors (INSTIs). This 3-quinolineacetic acid derivative series was identified using an enzymatic integrase long terminal repeat (LTR) DNA 3'-processing assay. A combination of medicinal chemistry, parallel synthesis, and structure-guided drug design led to the identification of BI 224436 as a candidate for preclinical profiling. It… CONTINUE READING
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