Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.

@article{Ben2010StudiesOT,
  title={Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.},
  author={Li Ben and Eric Dale Jones and Enkun Zhou and Chen Li and Dean Cameron Baylis and Shanghai Yu and Miao Wang and Xing He and Jonathan Alan Victor Coates and David Ian Rhodes and Gang Pei and John J. Deadman and Xin Xie and Dawei Ma},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 14},
  pages={4012-4}
}
A novel series of CCR5 antagonists has been identified, utilizing the lead, nifeviroc, which were further modified based on bioisosteric principles. Lead optimization was pursued by balancing potential toxicity and potency. Potent analogues with low toxic properties were successfully developed by formation of urea and amide bonds at the nitrogen at position… CONTINUE READING