title: Halogenated isoniazid derivatives VI. Evaluation of anti-HSV-1 and anti-HIV-1 in vitro activities of fluorinated analogues.
abstract: The synthesis and evaluation of antiviral in vitro activity are reported of some 2'-(1-arylethyl)isonicotinohydrazides (5a-d) and N-(1-arylethyl)isonicotinohydrazonic acids (6a-d), obtained by reducing fluorinated acetophenone isonicotinoylhydrazones (2a-d) with sodium cyanoborohydride. These INH analogues, along with other ones previously prepared, i.e. benzaldehyde isonicotinoylhydrazones 1, 4-aryl-1-methoxyl-1-(4-pyridyl)-2,3-diaza-1,3-butadienes 3 and 5-aryl-4-methyl-2-(4-pyridyl)-delta 2-1,3,4-oxadiazolines 4, were assayed for anti-HSV-1 activity on the monoblastoid cell line U937. Only some compounds (1b, 1d, 4d and 4e) displayed a moderate antiherpetic activity. In addition, the reduced compounds 5 and 6, submitted to the anti-HIV-1 screening, did not display significant effects in reducing virus-induced cytopathogenicity. The cytotoxicity of all compounds has been assayed on Vero cells and some considerations in correlation with structure are discussed.
authors.affiliation: Instituto di Microbiologia, Facoltà di Medicina e Chirurgia, Università di Messina, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Arena
authors.forename: A B
authors.initials: AB
authors.lastname: Capozza
authors.forename: R
authors.initials: R
authors.lastname: Maccari
authors.forename: R
authors.initials: R
authors.lastname: Ottanà
authors.forename: M G
authors.initials: MG
authors.lastname: Vigorita
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002522:Chlorocebus aethiops; D003470:Culture Media; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects*; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D006801:Humans; D007538:Isoniazid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013055:Spectrophotometry, Infrared; D013601:T-Lymphocytes / Q000187:drug effects / Q000821:virology; D014709:Vero Cells; D010948:Viral Plaque Assay
chemical_list: D000998:Antiviral Agents; D003470:Culture Media; D007538:Isoniazid