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[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains

Carta, Antonio and Palomba, Michele Francesco Luigi and Paglietti, Giuseppe and Molicotti, Paola and Paglietti, Bianca and Cannas, Sara and Zanetti, Stefania Anna Lucia (2007) [1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains. Bioorganic & Medicinal Chemistry Letters, Vol. 17 (17), p. 4791-4794. ISSN 0960-894X. Article.

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DOI: 10.1016/j.bmcl.2007.06.064

Abstract

In this preliminary study we report the activity of 3-methyl-9-substituted-6-oxo-6,9-dihydro-3H-[1,2,3]-triazolo[4,5-h]quinolone-carboxylic acids and their esters as a new class of antiinfective agents against MDR Mycobacterium tuberculosis. In antitubercular screening against H37Rv and 11 clinically isolated strains of M. tuberculosis several derivatives (1o,3a,c,i,j,p) showed MIC90 in the range 0.5–3.2 μg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC90 = 0.5 μg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.

Item Type:Article
ID Code:523
Status:Published
Refereed:Yes
Uncontrolled Keywords:Triazolo[4,5-h]quinolones, MDR M. tuberculosis, in vitro antitubercular 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:Pergamon-Elsevier Science
ISSN:0960-894X
Copyright Holders:© 2007 Elsevier Science
Deposited On:18 Aug 2009 10:02

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