4-Substituted anilino imidazo[1,2-a] and triazolo[4,3-a]quinoxalines. Synthesis and evaluation of in vitro biological activity.
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.
Corona
Paola
P
Dipartimento Farmaco Chimico Tossicologico, University of Sassari, Via Muroni 23/a, 07100 Sassari, Italy.
Vitale
Gabriella
G
Loriga
Mario
M
Paglietti
Giuseppe
G
La Colla
Paolo
P
Collu
Gabriella
G
Sanna
Giuseppina
G
Loddo
Roberta
R
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*
D007093:Imidazoles; D011810:Quinoxalines; D014230:Triazoles; C029899:imidazole