title: Synthesis and in vitro antimicrobial and antitumoral screening of novel lipophilic isoniazid analogues. VI.
abstract: Various kinds of lipophilic analogues of isonicotinic acid hydrazide (Isoniazid) were synthesized and in vitro explored in a search for antimycobacterial agents with extended activity spectrum against pathogens responsible for the AIDS-associated diseases. The primary in vitro screening showed that a) isonicotinoylhydrazones 1a, 1b, 1d, 1e are more active than the parent drug against non-tubercular mycobacteria (MIC ranging between 0.5 and 4 micrograms/ml), b) isonicotinohydrazides 6b and 6e display interesting antibacterial activity on some Gram + and Gram-strains, and c) trifluoromethyl-containing compounds 1a and 2c inhibit the growth of several human tumor cell lines at doses between 10(-5) and 10(-6) M. On the contrary, none of the tested analogues significantly counteracts the cytopathogenicity induced by HIV and HSV viruses.
authors.affiliation: Dipartimento Farmaco-chimico, Università di Messina, Italy.
authors.forename: M G
authors.initials: MG
authors.lastname: Vigorita
authors.forename: R
authors.initials: R
authors.lastname: Ottanà
authors.forename: R
authors.initials: R
authors.lastname: Maccari
authors.forename: F
authors.initials: F
authors.lastname: Monforte
authors.forename: G
authors.initials: G
authors.lastname: Bisignano
authors.forename: F C
authors.initials: FC
authors.lastname: Pizzimenti
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007538:Isoniazid / Q000031:analogs & derivatives*; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects; D014407:Tumor Cells, Cultured
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D007538:Isoniazid