Preprint Article Version 1 This version is not peer-reviewed

Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives

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. Preprints 2019, 2019020248 (doi: 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 (doi: 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.

Subject Areas

10-methoxycanthin-6-one; quaternization; antibacterial; SARs

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