Design, Synthesis and Biological Evaluation of Rose Bengal Analogues as SecA Inhibitors

Authors

  • Dr. Jianmei Cui,

    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302-4098 (USA)
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    • These authors contributed equally to this work.

  • Dr. Jinshan Jin,

    1. Department of Biology and Center for Diagnostics and Therapeutics, Georgia State University, P.O. Box 4010, Atlanta, GA 30302-4010 (USA)
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    • These authors contributed equally to this work.

  • Dr. Ying-Hsin Hsieh,

    1. Department of Biology and Center for Diagnostics and Therapeutics, Georgia State University, P.O. Box 4010, Atlanta, GA 30302-4010 (USA)
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  • Dr. Hsiuchin Yang,

    1. Department of Biology and Center for Diagnostics and Therapeutics, Georgia State University, P.O. Box 4010, Atlanta, GA 30302-4010 (USA)
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  • Dr. Bowen Ke,

    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302-4098 (USA)
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  • Dr. Krishna Damera,

    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302-4098 (USA)
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  • Dr. Phang C. Tai,

    Corresponding author
    1. Department of Biology and Center for Diagnostics and Therapeutics, Georgia State University, P.O. Box 4010, Atlanta, GA 30302-4010 (USA)
    • Department of Biology and Center for Diagnostics and Therapeutics, Georgia State University, P.O. Box 4010, Atlanta, GA 30302-4010 (USA)
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  • Dr. Binghe Wang

    Corresponding author
    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302-4098 (USA)
    • Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302-4098 (USA)
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Abstract

SecA, a key component of bacterial Sec-dependent secretion pathway, is an attractive target for exploring novel antimicrobials. Rose bengal (RB), a polyhalogenated fluorescein derivative, was found from our previous study as a potent SecA inhibitor. Here we describe the synthesis and structure–activity relationships (SAR) of 23 RB analogues that were designed by systematical dissection of RB. Evaluation of these analogues allowed us to establish an initial SAR in SecA inhibition. The antimicrobial effects of these SecA inhibitors are confirmed in experiments using E. coli and B. subtilis.

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