title: Potential new anti-human immunodeficiency virus type 1 compounds depress virus replication in cultured human macrophages.
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.
authors.affiliation: Biotron Limited, LPO Box A315, Eggleston Rd., Australian National University, Canberra, ACT 2601, Australia. gewart@biotron.com.au
authors.forename: Gary D
authors.initials: GD
authors.lastname: Ewart
authors.forename: Najla
authors.initials: N
authors.lastname: Nasr
authors.forename: Hassan
authors.initials: H
authors.lastname: Naif
authors.forename: Graeme B
authors.initials: GB
authors.lastname: Cox
authors.forename: Anthony L
authors.initials: AL
authors.lastname: Cunningham
authors.forename: Peter W
authors.initials: PW
authors.lastname: Gage
mesh_terms: D000584:Amiloride / Q000031:analogs & derivatives* / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004279:DNA, Viral / Q000096:biosynthesis / Q000235:genetics; D016655:HIV Core Protein p24 / Q000096:biosynthesis / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development; D054298:Human Immunodeficiency Virus Proteins; D006801:Humans; D008264:Macrophages / Q000187:drug effects / Q000821:virology*; D012367:RNA, Viral / Q000096:biosynthesis / Q000235:genetics; D054334:Viral Regulatory and Accessory Proteins / Q000096:biosynthesis; D014779:Virus Replication / Q000187:drug effects*; D000086082:Viroporin Proteins
chemical_list: D000584:Amiloride; D019380:Anti-HIV Agents; D004279:DNA, Viral; D016655:HIV Core Protein p24; D054298:Human Immunodeficiency Virus Proteins; D012367:RNA, Viral; D054334:Viral Regulatory and Accessory Proteins; C514859:vpu protein, Human immunodeficiency virus 1; D000086082:Viroporin Proteins; C057360:5-(N,N-hexamethylene)amiloride; C039465:5-dimethylamiloride