AUTHOR=Wu Wenneng , Lan Wenjun , Wu Chenyan , Fei Qiang 

TITLE=Synthesis and Antifungal Activity of Pyrimidine Derivatives Containing an Amide Moiety

JOURNAL=Frontiers in Chemistry

VOLUME=9

YEAR=2021

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2021.695628

DOI=10.3389/fchem.2021.695628

ISSN=2296-2646

ABSTRACT=<p>In this study, 17 novel pyrimidine derivatives containing an amide moiety were synthesized. Then their <italic>in vitro</italic> antifungal activities against <italic>Botryosphaeria dothidea</italic> (<italic>B. dothidea</italic>), <italic>Phomopsis</italic> sp., and <italic>Botrytis cinereal</italic> (<italic>B. cinereal</italic>) were determined. A preliminary biological test showed that compounds 5-bromo-2-fluoro<italic>-N</italic>-(2-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (<bold>5f</bold>) and 5-bromo-2-fluoro-<italic>N</italic>-(3-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (<bold>5o</bold>) exhibited higher antifungal activity against <italic>Phomopsis</italic> sp., with an inhibition rate of 100% compared to that of Pyrimethanil at 85.1%. In particular, compound <bold>5o</bold> exhibited excellent antifungal activity against <italic>Phompsis</italic> sp., with the EC<sub>50</sub> value of 10.5 μg/ml, which was even better than that of Pyrimethanil (32.1 μg/ml). As far as we know, this is the first report on the antifungal activities against <italic>B. dothidea</italic>, <italic>Phomopsis</italic> sp., and <italic>B. cinereal</italic> of this series of pyrimidine derivatives containing an amide moiety.</p>