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

Bibliographic Details
Title: Synthesis and Evaluation of Ester Derivatives of 10-Hydroxycanthin-6-one as Potential Antimicrobial Agents
Authors: Fei Zhao, Jiang-Kun Dai, Dan Liu, Shi-Jun Wang, Jun-Ru Wang
Source: Molecules, Vol 21, Iss 3, p 390 (2016)
Publisher Information: MDPI AG, 2016.
Publication Year: 2016
Collection: LCC:Organic chemistry
Subject Terms: 10-hydroxycanthin-6-one, ester derivatives, antibacterial activity, antifungal activity, Organic chemistry, QD241-441
More Details: 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.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 1420-3049
Relation: http://www.mdpi.com/1420-3049/21/3/390; https://doaj.org/toc/1420-3049
DOI: 10.3390/molecules21030390
Access URL: https://doaj.org/article/41a59b79b701432bb96f0802244dbf21
Accession Number: edsdoj.41a59b79b701432bb96f0802244dbf21
Database: Directory of Open Access Journals
More Details
ISSN:14203049
DOI:10.3390/molecules21030390
Published in:Molecules
Language:English