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

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

  • Bioorg Med Chem Lett. 2010 Jul 15;20(14):4012-4. doi: 10.1016/j.bmcl.2010.05.102.
Li Ben 1,  Eric Dale Jones,  Enkun Zhou,  Chen Li,  Dean Cameron Baylis,  Shanghai Yu,  Miao Wang,  Xing He,  Jonathan Alan Victor Coates,  David Ian Rhodes,  Gang Pei,  John Joseph Deadman,  Xin Xie,  Dawei Ma
Affiliations

Affiliation

  • 1 Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 319 Yueyang Lu, Shanghai 200031, China.
PMID: 20561788 DOI: 10.1016/j.bmcl.2010.05.102
Abstract

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 4- of the pyrrolidine ring.

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