Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.

@article{Fader2014MinimizingTC,
  title={Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.},
  author={Lee D. Fader and Rebekah J. Carson and S{\'e}bastien Morin and François Bilodeau and Catherine Chabot and Ted Halmos and Murray D. Bailey and Stephen H. Kawai and R. H. Coulombe and Steven R LaPlante and Kevork Mekhssian and Araz Jakalian and Michel Garneau and Jianmin Duan and Stephen W. Mason and Bruno Simoneau and Craig Fenwick and Youla S Tsantrizos and Christiane Yoakim},
  journal={ACS medicinal chemistry letters},
  year={2014},
  volume={5 6},
  pages={
          711-6
        }
}
A scaffold replacement approach was used to identifying the pyridine series of noncatalytic site integrase inhibitors. These molecules bind with higher affinity to a tetrameric form compared to a dimeric form of integrase. Optimization of the C6 and C4 positions revealed that viruses harboring T124 or A124 amino acid substitutions are highly susceptible to these inhibitors, but viruses having the N124 amino acid substitution are about 100-fold less susceptible. Compound 20 had EC50 values <10… CONTINUE READING

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