Potential new anti-human immunodeficiency virus type 1 compounds depress virus replication in cultured human macrophages

Antimicrob Agents Chemother. 2004 Jun;48(6):2325-30. doi: 10.1128/AAC.48.6.2325-2330.2004.

Abstract

We report that the amiloride analogues 5-(N,N-hexamethylene)amiloride and 5-(N,N-dimethyl)amiloride inhibit, at micromolar concentrations, the replication of human immunodeficiency virus type 1 (HIV-1) in cultured human blood monocyte-derived macrophages. These compounds also inhibit the in vitro activities of the HIV-1 Vpu protein and might represent lead compounds for a new class of anti-HIV-1 drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amiloride / analogs & derivatives*
  • Amiloride / pharmacology*
  • Anti-HIV Agents / pharmacology*
  • Cell Division / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • DNA, Viral / biosynthesis
  • DNA, Viral / genetics
  • HIV Core Protein p24 / biosynthesis
  • HIV Core Protein p24 / genetics
  • HIV-1 / drug effects*
  • HIV-1 / growth & development
  • Human Immunodeficiency Virus Proteins
  • Humans
  • Macrophages / drug effects
  • Macrophages / virology*
  • RNA, Viral / biosynthesis
  • RNA, Viral / genetics
  • Viral Regulatory and Accessory Proteins / biosynthesis
  • Virus Replication / drug effects*

Substances

  • Anti-HIV Agents
  • DNA, Viral
  • HIV Core Protein p24
  • Human Immunodeficiency Virus Proteins
  • RNA, Viral
  • Viral Regulatory and Accessory Proteins
  • vpu protein, Human immunodeficiency virus 1
  • 5-(N,N-hexamethylene)amiloride
  • 5-dimethylamiloride
  • Amiloride