Format

Send to

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2007 Sep 1;17(17):4791-4. Epub 2007 Jun 26.

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

Author information

1
Dipartimento Farmaco Chimico Tossicologico, Università degli Studi di Sassari, Via Muroni 23/a, 07100, Sassari, Italy. acarta@uniss.it

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 MIC(90) in the range 0.5-3.2 microg/mL. 3c showed no cytotoxicity and proved to be the most potent derivative exhibiting MIC(90)=0.5 microg/mL against all M. tuberculosis strains and infected human macrophages (J774-A1) tested.

PMID:
17604166
DOI:
10.1016/j.bmcl.2007.06.064
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Support Center