AUTHOR=Lan Wenjun , Tang Xuemei , Yu Jia , Fei Qiang , Wu Wenneng , Li Pei , Luo Heng 

TITLE=Design, Synthesis, and Bioactivities of Novel Trifluoromethyl Pyrimidine Derivatives Bearing an Amide Moiety

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.952679

DOI=10.3389/fchem.2022.952679

ISSN=2296-2646

ABSTRACT=<p>Twenty-three novel trifluoromethyl pyrimidine derivatives containing an amide moiety were designed and synthesized through four-step reactions and evaluated for their antifungal, insecticidal, and anticancer properties. Bioassay results indicated that some of the title compounds exhibited good <italic>in vitro</italic> antifungal activities against <italic>Botryosphaeria dothidea</italic> (<italic>B. dothidea</italic>), <italic>Phompsis</italic> sp., <italic>Botrytis cinereal</italic> (<italic>B. cinerea</italic>), <italic>Colletotrichum gloeosporioides</italic> (<italic>C. gloeosporioides</italic>), <italic>Pyricutaria oryzae</italic> (<italic>P. oryzae</italic>), and <italic>Sclerotinia sclerotiorum</italic> (<italic>S. sclerotiorum</italic>) at 50 μg/ml. Meanwhile, the synthesized compounds showed moderate insecticidal activities against <italic>Mythimna separata</italic> (<italic>M. separata</italic>) and <italic>Spdoptera frugiperda</italic> (<italic>S. frugiperda</italic>) at 500 μg/ml, which were lower than those of chlorantraniliprole. In addition, the synthesized compounds indicated certain anticancer activities against PC3, K562, Hela, and A549 at 5 μg/ml, which were lower than those of doxorubicin. Notably, this work is the first report on the antifungal, insecticidal, and anticancer activities of trifluoromethyl pyrimidine derivatives bearing an amide moiety.</p>