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    In Vitro and In Vivo Evaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness

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    Wenzler_in_vitro2014.pdf (619.4Kb)
    Issue Date
    2014-05-27
    Author
    Wenzler, Tanja
    Yang, Sihyung
    Patrick, Donald A.
    Braissant, Olivier
    Ismail, Mohamed A.
    Tidwell, Richard R.
    Boykin, David W.
    Wang, Zhuo
    Brun, Reto
    Publisher
    American Society for Microbiology
    Type
    Article
    Article Version
    Scholarly/refereed, publisher version
    Published Version
    10.1128/AAC.02309-13
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    Abstract
    African sleeping sickness is a neglected tropical disease transmitted by tsetse flies. New and better drugs are still needed especially for its second stage, which is fatal if untreated. 28DAP010, a dipyridylbenzene analogue of DB829, is the second simple diamidine found to cure mice with central nervous system infections by a parenteral route of administration. 28DAP010 showed efficacy similar to that of DB829 in dose-response studies in mouse models of first- and second-stage African sleeping sickness. The in vitro time to kill, determined by microcalorimetry, and the parasite clearance time in mice were shorter for 28DAP010 than for DB829. No cross-resistance was observed between 28DAP010 and pentamidine on the tested Trypanosoma brucei gambiense isolates from melarsoprol-refractory patients. 28DAP010 is the second promising preclinical candidate among the diamidines for the treatment of second-stage African sleeping sickness.
    Description
    This is the published version.
    URI
    http://hdl.handle.net/1808/19370
    Collections
    • Pharmacy Scholarly Works [286]
    Citation
    Wenzler, T., S. Yang, D. A. Patrick, O. Braissant, M. A. Ismail, R. R. Tidwell, D. W. Boykin, M. Z. Wang, and R. Brun. "In Vitro and In Vivo Evaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness." Antimicrobial Agents and Chemotherapy 58.8 (2014): 4452-463. http://dx.doi.org/10.1128/AAC.02309-13

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    KU Libraries
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    KU Libraries
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    Lawrence, KS 66045
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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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