Novel pyrimidine derivatives containing an amide moiety: design, synthesis, and antifungal activity

Abstract

The objectives of the current study were to synthesize a series of novel pyrimidine derivatives containing an amide moiety and to investigate their in vitro antifungal activities against eight kinds of plant pathogenic fungi via the poison plate technique. The preliminary biological test showed that compounds 4a–4aa exhibited moderate-to-good antifungal activities against the tested plant pathogenic fungi compared with the commercial agents. Particularly, compounds 4n, 4q, and 4w exhibited excellent antifungal activity against Phomopsis sp., with the half-maximal effective concentration (EC50) values of 1.8, 1.4, and 1.7 μg/mL, which were even better than that of pyrimethanil (32.1 μg/mL). To the best of our knowledge, this is the first report on the antifungal activity of this series of novel N-acyl 4-(4-aminophenoxy)-2-methyl-6-trifluoromethylpyrimidine derivatives containing an amide moiety.