Literature DB >> 16420032

Targeting FtsZ for antituberculosis drug discovery: noncytotoxic taxanes as novel antituberculosis agents.

Qing Huang1, Fumiko Kirikae, Teruo Kirikae, Antonella Pepe, Amol Amin, Laurel Respicio, Richard A Slayden, Peter J Tonge, Iwao Ojima.   

Abstract

Screening of 120 taxanes identified a number of compounds that exhibited significant antituberculosis activity. Rational optimization of selected compounds led to the discovery that the C-seco-taxane-multidrug-resistance (MDR) reversal agents (C-seco-TRAs) are noncytotoxic at the upper limit of solubility and detection (>80 microM), while maintaining MIC(99) values of 1.25-2.5 microM against drug-resistant and drug-sensitive strains of Mycobacterium tuberculosis (MTB). Treatment of MTB cells with TRA 3aa and 10a at the MIC caused filamentation and prolongation of the cells, a phenotypic response to FtsZ inactivation.

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Year:  2006        PMID： 16420032      PMCID： PMC2527599          DOI： 10.1021/jm050920y

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

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  9 in total
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