Version 1
: Received: 26 February 2019 / Approved: 27 February 2019 / Online: 27 February 2019 (05:08:02 CET)
How to cite:
Li, N.; Dai, J.; Liu, D.; Wang, J.; Wang, J. Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives. Preprints2019, 2019020248. https://doi.org/10.20944/preprints201902.0248.v1
Li, N.; Dai, J.; Liu, D.; Wang, J.; Wang, J. Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives. Preprints 2019, 2019020248. https://doi.org/10.20944/preprints201902.0248.v1
Li, N.; Dai, J.; Liu, D.; Wang, J.; Wang, J. Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives. Preprints2019, 2019020248. https://doi.org/10.20944/preprints201902.0248.v1
APA Style
Li, N., Dai, J., Liu, D., Wang, J., & Wang, J. (2019). Synthesis and <em>in vitro</em> Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives. Preprints. https://doi.org/10.20944/preprints201902.0248.v1
Chicago/Turabian Style
Li, N., Jin-Yi Wang and Jun-Ru Wang. 2019 "Synthesis and <em>in vitro</em> Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives" Preprints. https://doi.org/10.20944/preprints201902.0248.v1
Abstract
Natural products are an important source of antibacterial agents. Canthin-6-one alkaloids have displayed potential antibacterial activity based on our previous work. In order to improve the activity, twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by double dilution method. Four compounds (6f, 6i, 6p and 6t) displayed 2-fold superiority (minimum inhibitory concentration (MIC) = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae than agrochemical propineb. Moreover, the structure–activity relationships (SARs) were also carefully summarized in order to guide the development of antibacterial canthin-6-one agents.
Chemistry and Materials Science, Medicinal Chemistry
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
