AUTHOR=Xie Dandan , Yang Zaiping , Hu Xin , Wen Yin 

TITLE=Synthesis, Antibacterial and Insecticidal Activities of Novel Capsaicin Derivatives Containing a Sulfonic Acid Esters Moiety

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.929050

DOI=10.3389/fchem.2022.929050

ISSN=2296-2646

ABSTRACT=<p>In order to develop an efficient and broad-spectrum bactericide, a series of novel capsaicin derivatives containing a sulfonic acid esters moiety was synthesized. The structure of these compounds were confirmed by nuclear magnetic resonance spectroscopy (NMR) and high-resolution mass spectrum (HRMS). The results of the bioactivities revealed that some target compounds exhibited remarkable antibacterial activity. Compound <bold>3b</bold> exhibited the highest activities against <italic>Pseudomonas syringae</italic> pv. <italic>actinidiae</italic> (Psa), <italic>Xanthomonas oryzae</italic> pv. <italic>oryzae</italic> (Xoo), and <italic>Xanthomonas axonopodis</italic> pv. <italic>citri</italic> (Xac), and the values were 86, 54, and 92% at 50 μg/ml, respectively, which were higher than were for thiodiazole copper (87, 34, and 77%) and bismerthiazol (87, 37 and 75%). Although some compounds also showed certain activity against <italic>Spodoptera frugiperda</italic>, it was weaker than the positive controls monosultap and mulfoxaflor. Thus, the bioassay results recommend that these newly designed and synthesized scaffolds should be used as a bactericide lead compound rather than an insecticide lead compound.</p>