Synthesis and Antifungal Activities of Some Novel Pyrimidine Derivatives

Li Sun,Min Luo,Lingzi Zhang,Jie Wu,Dequn Sun

doi:10.3390/molecules16075618

Li Sun, Min Luo + Show 3 more

Open Access

https://doi.org/10.3390/molecules16075618

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Journal: Molecules (Basel, Switzerland)	Publication Date: Jun 30, 2011
Citations: 52	License type: CC BY 3.0

Affiliation: Shandong University

Abstract

Three series of new pyrimidine derivatives were synthesized and their antifungal activities were evaluated in vitro against fourteen phytopathogenic fungi. The results indicated that most of the synthesized compounds possessed fungicidal activities and some of them are more potent than the control fungicides. Preliminary SAR was also discussed.

Highlights

Phytopathogenic fungi that infect many crops are hard to control and risk resistance to the widely used commercial fungicides [1], there is a continuous need for new classes of antifungal agents
All of the new compounds were evaluated in vitro for their antifungal activities against fourteen phytopathogenic fungi and the results of preliminary bioassays were compared with those of some commercial agricultural fungicides: flumorph, dimethomorph, carbendazim, hymexazole and pyrimethanil (Figure 1), which were currently used in the field in China
Compounds 2a and 2b were obtained according to the similar method in literature [15] in the presence of KI

Summary

Introduction

Phytopathogenic fungi that infect many crops are hard to control and risk resistance to the widely used commercial fungicides [1], there is a continuous need for new classes of antifungal agents. Three series of new pyrimidine derivatives 1–4 were designed and synthesized. The synthetic routes are shown in Scheme 1. All of the new compounds were evaluated in vitro for their antifungal activities against fourteen phytopathogenic fungi and the results of preliminary bioassays were compared with those of some commercial agricultural fungicides: flumorph, dimethomorph, carbendazim, hymexazole and pyrimethanil (Figure 1), which were currently used in the field in China. The results indicated that most of the pyrimidine derivatives possessed certain fungicidal activities, and the preliminary SAR of these compounds was investigated. Synthetic routes to the three series of pyrimidine derivatives

Synthesis

Antifungal Bioassay

General

Procedures for the Preparation of Title Compounds 1–4

Conclusions