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Molecules 2016, 21(3), 390;

Synthesis and Evaluation of Ester Derivatives of 10-Hydroxycanthin-6-one as Potential Antimicrobial Agents

College of Science, Northwest A & F University, Yangling 712100, China
Author to whom correspondence should be addressed.
Academic Editors: Shufeng Zhou and Wei-Zhu Zhong
Received: 22 February 2016 / Revised: 12 March 2016 / Accepted: 16 March 2016 / Published: 21 March 2016
(This article belongs to the Special Issue Drug Design and Discovery: Principles and Applications)
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As part of our continuing research on canthin-6-one antimicrobial agents, a new series of ester derivatives of 10-hydroxycanthin-6-one were synthesized using a simple and effective synthetic route. The structure of each compound was characterized by NMR, ESI-MS, FT-IR, UV, and elemental analysis. The antimicrobial activity of these compounds against three phytopathogenic fungi (Alternaria solani, Fusarium graminearum, and Fusarium solani) and four bacteria (Bacillus cereus, Bacillus subtilis, Ralstonia solanacearum, and Pseudomonas syringae) were evaluated using the mycelium linear growth rate method and micro-broth dilution method, respectively. The structure-activity relationship is discussed. Of the tested compounds, 4 and 7s displayed significant antifungal activity against F. graminearum, with inhibition rates of 100% at a concentration of 50 μg/mL. Compounds 5, 7s, and 7t showed the best inhibitory activity against all the tested bacteria, with minimum inhibitory concentrations (MICs) between 3.91 and 31.25 μg/mL. Thus, 7s emerged as a promising lead compound for the development of novel canthine-6-one antimicrobial agents. View Full-Text
Keywords: 10-hydroxycanthin-6-one; ester derivatives; antibacterial activity; antifungal activity 10-hydroxycanthin-6-one; ester derivatives; antibacterial activity; antifungal activity

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Zhao, F.; Dai, J.-K.; Liu, D.; Wang, S.-J.; Wang, J.-R. Synthesis and Evaluation of Ester Derivatives of 10-Hydroxycanthin-6-one as Potential Antimicrobial Agents. Molecules 2016, 21, 390.

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