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Synthesis, anti-mycobacterial, anti-trichomonas and anti-candida in vitro activities of 2-substituted-6,7-difluoro-3-methylquinoxaline 1,4-dioxides

Carta, Antonio and Loriga, Mario and Paglietti, Giuseppe and Mattana, Antonella and Fiori, Pier Luigi and Molicotti, Paola and Sechi, Leonardo Antonio and Zanetti, Stefania Anna Lucia (2004) Synthesis, anti-mycobacterial, anti-trichomonas and anti-candida in vitro activities of 2-substituted-6,7-difluoro-3-methylquinoxaline 1,4-dioxides. European Journal of Medicinal Chemistry, Vol. 39 (2), p. 195-203. ISSN 0223-5234. Article.

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DOI: 10.1016/j.ejmech.2003.11.008

Abstract

A new series of 23 6,7-difluoro-3-methyl-2-phenylthio/phenylsulfonyl/phenylsulfinyl/benzylamino/phenylamino-quinoxaline 1,4-dioxides variously substituted in the phenyl moiety, was synthesized and submitted to in vitro evaluation for anti-mycobacterial, anti-trichomonas, anti-candida, anti-mycoplasma and antibacterial activities. In anti-mycobacterial assays, several compounds resulted active (MIC90 = 2.0–4.0 μg/ml) against Mycobacterium tuberculosis H37Rv. Anti-trichomonas screening showed a generally good activity of all compounds (MBC = 0.39–25.0 μg/ml) versus Trichomonas vaginalis, in particular the derivatives 5a,d, 7a, 9 and 11c ranged 0.39–0.78 μg/ml (metronidazole MBC = 12.5 μg/ml). Results of anti-candida assays showed that derivatives 7a, 8a,d and 9 were active against several species of Candida (C. albicans, C. krusei, C. parapsilosis and C. glabrata), having MIC50 between 3.9 and 31.25 μg/ml. The latter compounds were also submitted to anti-mycoplasma assay against Mycoplasma hominis, the results obtained showed that 7a, 8a,d and 9 inhibited the growth of the mycoplasma at the concentration of 0.1 mg/ml. In antibacterial tests only a few compounds showed an MIC50 lower than 62.5 μg/ml against representative strains of Gram-positive and Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Vibrio alginolyticus and Pseudomonas aeruginosa).

Item Type:Article
ID Code:533
Status:Published
Refereed:Yes
Uncontrolled Keywords:Quinoxaline 1,4-dioxides, anti-mycobacterial, anti-trichomonas, anti-candida activity, SAR
Subjects:Area 06 - Scienze mediche > MED/07 Microbiologia e microbiologia clinica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze biomediche
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier Masson
ISSN:0223-5234
Copyright Holders:© 2003 Elsevier
Deposited On:18 Aug 2009 10:02

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