Synthesis, biological activity, and ADME properties of novel S-DABOs/N-DABOs as HIV reverse transcriptase inhibitors.

@article{Radi2012SynthesisBA,
  title={Synthesis, biological activity, and ADME properties of novel S-DABOs/N-DABOs as HIV reverse transcriptase inhibitors.},
  author={Marco Radi and Mafalda Pagano and L. Franchi and Daniele Castagnolo and Silvia Schenone and Gianni Casaluce and Claudio Zamperini and Elena Dreassi and Giovanni Maga and Alberta Samuele and Encarna Gonzalo and Bonaventura Clotet and Jos{\'e} A. Est{\'e} and Maurizio Botta},
  journal={ChemMedChem},
  year={2012},
  volume={7 5},
  pages={883-96}
}
Previous studies aimed at exploring the SAR of C2-functionalized S-DABOs demonstrated that the substituent at this position plays a key role in the inhibition of both wild-type RT and drug-resistant enzymes, particularly the K103N mutant form. The introduction of a cyclopropyl group led us to the discovery of a potent inhibitor with picomolar activity against wild-type RT and nanomolar activity against many key mutant forms such as K103N. Despite its excellent antiviral profile, this compound… CONTINUE READING