Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.

@article{Zhao2016IncorporationOP,
  title={Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.},
  author={Yu Zhao and Qiong Gu and Susan Lynne Morris-Natschke and Chin-ho Chen and Kuo-Hsiung Lee},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 19},
  pages={
          9262-9268
        }
}
Two "privileged fragments", caffeic acid and piperazine, were integrated into bevirimat producing new derivatives with improved activity against HIV-1/NL4-3 and NL4-3/V370A carrying the most prevalent bevirimat-resistant polymorphism. The activity of one of these, 18c, was increased by 3-fold against NL4-3 and 51-fold against NL4-3/V370A. Moreover, 18c is a maturation inhibitor with improved metabolic stability. Our study suggested that integration of privileged motifs into promising natural… CONTINUE READING