Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4753-6. doi: 10.1016/j.bmcl.2010.06.135. Epub 2010 Jul 1.

Abstract

The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology
  • CCR5 Receptor Antagonists*
  • Humans
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Receptors, CCR5 / metabolism
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Pyrazoles
  • Receptors, CCR5