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Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity

Carta, Antonio and Paglietti, Giuseppe and Rhabar Nikookar, Mohammad E. and Sanna, Paolo Antonio and Sechi, Leonardo Antonio and Zanetti, Stefania Anna Lucia (2002) Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity. European Journal of Medicinal Chemistry, Vol. 37 (5), p. 355-366. ISSN 0223-5234. Article.

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DOI: 10.1016/S0223-5234(02)01346-6

Abstract

Thirty-six 6(7)-substituted-3-methyl- or 3-halogenomethyl-2-phenylthio–phenylsulphonyl–chloro-quinoxaline 1,4-dioxides belonging to series 3–6 were synthesised and submitted to a preliminary in vitro evaluation for antimycobacterial, anticandida and antibacterial activities. Antitubercular screening showed a generally good activity of 3-methyl-2-phenylthioquinoxaline 1,4-dioxides (3d,e,h–j) against Mycobacterium tuberculosis, and exhibited MIC between 0.39 and 0.78 μg mL−1 (rifampicin MIC=0.25 μg mL−1), whereas in compounds 4d,e, 5a,b,d,e,l and 6b–e,j,l MIC ranged between 1.56 and 6.25 μg mL−1. Results of the antibacterial and anticandida screening showed that 6e and 6l exhibited MIC=0.4 and 1.9 μg mL−1, respectively, against Candida krusei (miconazole MIC=0.9 μg mL−1), and 4i, 5b,d, 6e, MIC=3.9 μg mL−1 against Candida glabrata (miconazole MIC=0.4 μg mL−1), while compounds 3d,l, 5e,l, and 6b,d,e,l showed MIC=15.6 μg mL−1 against Vibrio alginolyticus.

Item Type:Article
ID Code:543
Status:Published
Refereed:Yes
Uncontrolled Keywords:Quinoxaline 1,4-dioxides, antimycobacterial, anticandida, antibacterial activity
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:© 2002 Éditions scientifiques et médicales Elsevier
Deposited On:18 Aug 2009 10:02

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