Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties
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- 作者：Jun-Jie Koha ; b ; Hanxun Zoua ; Devika Mukherjeec ; Shuimu Lina ; Fanghui Lima ; Javey Khiapeng Tana ; Dhi-Zen Tana ; Bridget L. Stockerg ; Mattie S.M. Timmerh ; Hilary M. Corkrang ; h ; Rajamani Lakshminarayanana ; e ; Donald T.H. Tand ; Derong Caof ; Roger W. Beuermana ; e ; rwbeuerman@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Thomas Dickc ; thomas_dick@nuhs.edu.sg" class="auth_mail" title="E-mail the corresponding author ; Shouping Liua ; e ; liushouping@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Mycobacteria ; Tuberculosis ; Xanthone ; Membrane targeting
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：684-703
- 全文大小：3044 K
文摘
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The structure-activity relationships of the amphiphilic xanthones against mycobacteria are explored.
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Amphiphilic xanthones are active against Mycobacterium tuberculosis and no cross-resistance to 1st line anti-mycobacterial agents.
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Anti-mycobacterial action of the amphiphilic xanthones involves inner membrane disruption and ATP depletion.
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In vitro and In vivo pharmacokinetics of the amphiphilic xanthone derivatives is explored.