1. Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones.
- Author
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Pasca MR, Degiacomi G, Ribeiro AL, Zara F, De Mori P, Heym B, Mirrione M, Brerra R, Pagani L, Pucillo L, Troupioti P, Makarov V, Cole ST, and Riccardi G
- Subjects
- Base Sequence, DNA Primers genetics, DNA, Bacterial genetics, Drug Resistance, Multiple, Bacterial genetics, Europe, Genes, Bacterial, Humans, In Vitro Techniques, Microbial Sensitivity Tests, Mutation, Mycobacterium tuberculosis enzymology, Mycobacterium tuberculosis genetics, Racemases and Epimerases genetics, Antitubercular Agents pharmacology, Mycobacterium tuberculosis drug effects, Mycobacterium tuberculosis isolation & purification, Spiro Compounds pharmacology, Thiazines pharmacology, Tuberculosis, Multidrug-Resistant drug therapy, Tuberculosis, Multidrug-Resistant microbiology
- Abstract
The new antitubercular drug candidate 2-[2-S-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one (BTZ043) targets the DprE1 (Rv3790) subunit of the enzyme decaprenylphosphoryl-beta-d-ribose 2'-epimerase. To monitor the potential development of benzothiazinone (BTZ) resistance, a total of 240 sensitive and multidrug-resistant Mycobacterium tuberculosis clinical isolates from four European hospitals were surveyed for the presence of mutations in the dprE1 gene and for BTZ susceptibility. All 240 strains were susceptible, thus establishing the baseline prior to the introduction of BTZ043 in clinical trials.
- Published
- 2010
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