title: Halogenated isoniazid derivatives as possible antimycobacterial and anti-HIV agents--III.
abstract: As part of a research directed to the synthesis of novel isoniazid derivatives with potential activity on mycobacteria and HIV virus, the acetophenone-isonicotinoylhydrazones 3 and the 4-aryl-1-methoxy-1-(4-pyridyl)- 2,3-diaza-1,3-butadienes 5, obtained by reaction between isonicotinoylhydrazones and diazomethane, have been prepared and tested for such activities. Both classes of derivatives showed interesting growth inhibitory activity on non-tubercular mycobacteria, including the emerging M. avium. Such activity appears to be linked to fluorine and/or chlorine presence on benzene rings. In contrast, none of the compounds submitted to the anti-AIDS in vitro screening, displayed any protection against HIV-1 virus-induced cytopathic effect in T4-lymphocyte cell lines.
authors.affiliation: Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Villaggio SS. Annunziata, Messina, Italy.
authors.forename: M G
authors.initials: MG
authors.lastname: Vigorita
authors.forename: R
authors.initials: R
authors.lastname: Ottanà
authors.forename: C
authors.initials: C
authors.lastname: Zappalà
authors.forename: R
authors.initials: R
authors.lastname: Maccari
authors.forename: F C
authors.initials: FC
authors.lastname: Pizzimenti
authors.forename: G
authors.initials: G
authors.lastname: Gabbrielli
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D006678:HIV / Q000187:drug effects*; D006846:Hydrocarbons, Halogenated / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007538:Isoniazid / Q000031:analogs & derivatives*; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D006846:Hydrocarbons, Halogenated; D007538:Isoniazid