Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3103-6. doi: 10.1016/s0960-894x(01)00655-2.

Abstract

Replacement of the large hydantoin-indole moiety from our previous work with a variety of smaller heterocyclic analogues gave rise to potent CCR5 antagonists having binding affinity comparable to the hydantoin analogues. The synthesis, SAR, and biological profiles of this class of antagonists are described.

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Anti-HIV Agents / therapeutic use*
  • CCR5 Receptor Antagonists*
  • HIV Infections / drug therapy*
  • HIV-1 / isolation & purification
  • HeLa Cells
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology
  • Heterocyclic Compounds / therapeutic use*
  • Humans
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Heterocyclic Compounds