title: 4-Substituted anilino imidazo[1,2-a] and triazolo[4,3-a]quinoxalines. Synthesis and evaluation of in vitro biological activity.
abstract: Fifteen imidazo[1,2-a] and [1,2,4]triazolo[4,3-a]quinoxalines were prepared. These compounds bear at position 4 various substituents related to the moieties present in classical and non-classical antifolic agents. And we evaluated in vitro antimicrobial, antiviral and antiproliferative activities. In particular, title compounds were evaluated in vitro against representative strains of Gram-positive and Gram-negative bacteria (S. aureus, Salmonella spp.), mycobacteria (M. fortuitum, M. smegmatis ATCC 19420 and M. tuberculosis ATCC 27294), yeast and moulds (C. albicans ATCC 10231 and A. fumigatus). Furthermore, their antiretroviral activity against HIV-1 was determined in MT-4 cells together with cytotoxicity. In these assays title compounds were tested for their capability to prevent MT-4 cell growth. Among the examined series, the compounds 5, 7 and 10 showed cytotoxicity against mock-infected MT-4 cells.
authors.affiliation: Dipartimento Farmaco Chimico Tossicologico, University of Sassari, Via Muroni 23/a, 07100 Sassari, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Corona
authors.forename: Gabriella
authors.initials: G
authors.lastname: Vitale
authors.forename: Mario
authors.initials: M
authors.lastname: Loriga
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Paglietti
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Gabriella
authors.initials: G
authors.lastname: Collu
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Roberta
authors.initials: R
authors.lastname: Loddo
mesh_terms: D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D015394:Molecular Structure; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry*
chemical_list: D007093:Imidazoles; D011810:Quinoxalines; D014230:Triazoles; C029899:imidazole