1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2997-3000. doi: 10.1016/s0960-894x(02)00605-4.

Abstract

Incorporation of acidic functional groups into a lead CCR5 antagonist identified from a targeted combinatorial library resulted in compounds with enhanced anti-HIV-1 activity and attenuated L-type calcium channel affinity.

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology*
  • CCR5 Receptor Antagonists*
  • CHO Cells
  • Calcium Channels, L-Type / drug effects
  • Chemical Phenomena
  • Chemistry, Physical
  • Chemokine CCL4
  • Cricetinae
  • HIV-1 / drug effects*
  • Half-Life
  • HeLa Cells
  • Humans
  • Macrophage Inflammatory Proteins / antagonists & inhibitors
  • Rats
  • Receptors, CCR5 / chemistry
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Calcium Channels, L-Type
  • Chemokine CCL4
  • Macrophage Inflammatory Proteins
  • Receptors, CCR5