Novel Pyrimidine Derivatives Bearing a 1,3,4-Thiadiazole Skeleton: Design, Synthesis, and Antifungal Activity

Nianjuan Pan; Chunyi Liu; Ruirui Wu; Qiang Fei; Wenneng Wu

doi:10.3389/fchem.2022.922813

Novel Pyrimidine Derivatives Bearing a 1,3,4-Thiadiazole Skeleton: Design, Synthesis, and Antifungal Activity

Front Chem. 2022 Jun 8:10:922813. doi: 10.3389/fchem.2022.922813. eCollection 2022.

Authors

Nianjuan Pan¹, Chunyi Liu¹, Ruirui Wu¹, Qiang Fei¹, Wenneng Wu¹

Affiliation

¹ Food and Pharmaceutical Engineering Institute, Guiyang University, Guiyang, China.

Abstract

In this study, twenty novel pyrimidine derivatives bearing a 1,3,4-thiadiazole skeleton were designed and synthesized. Then their antifungal activity against Botrytis cinereal (B. cinereal), Botryosphaeria dothidea (B. dothidea), and Phomopsis sp. were determined using the poison plate technique. Biological test results showed that compound 6h revealed lower EC₅₀ values (25.9 and 50.8 μg/ml) on Phompsis sp. than those of pyrimethanil (32.1 and 62.8 μg/ml).

Keywords: 4-thiadiazole; antifungal activity; design; pyrimidine; synthesis.