Halogenated isoniazid derivatives as possible antimycobacterial and anti-HIV agents--III.
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.
Vigorita
M G
MG
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Villaggio SS. Annunziata, Messina, Italy.
Ottanà
R
R
Zappalà
C
C
Maccari
R
R
Pizzimenti
F C
FC
Gabbrielli
G
G
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
D000998:Antiviral Agents; D006846:Hydrocarbons, Halogenated; D007538:Isoniazid