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4-Substituted anilino imidazo[1,2-a] and triazolo[4,3-a]quinoxalines: synthesis and evaluation of in vitro biological activity

Corona, Paola and Vitale, Gabriella and Loriga, Mario and Paglietti, Giuseppe and La Colla, Paolo and Collu, Gabriella and Sanna, Giuseppina and Loddo, Roberta (2006) 4-Substituted anilino imidazo[1,2-a] and triazolo[4,3-a]quinoxalines: synthesis and evaluation of in vitro biological activity. European Journal of Medicinal Chemistry, Vol. 41 (9), p. 1102-1107. ISSN 0223-5234. Article.

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DOI: 10.1016/j.ejmech.2006.05.015

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.

Item Type:Article
ID Code:528
Status:Published
Refereed:Yes
Uncontrolled Keywords:Imidazo[1,2-a]quinoxalines, triazolo[4,3-a]quinoxalines, biological activity
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier Masson
ISSN:0223-5234
Copyright Holders:© 2006 Elsevier
Deposited On:18 Aug 2009 10:02

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