synthesis and antifungal activities of some novel pyrimidine derivatives合成和抗真菌的活动一些新奇的嘧啶衍生品.pdfVIP

Molecules 2011, 16, 5618-5628; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Communication Synthesis and Antifungal Activities of Some Novel Pyrimidine Derivatives Li Sun, Jie Wu, Lingzi Zhang, Min Luo and Dequn Sun * Marine College, Shandong University, Weihai Wenhua West Road, No.180, Weihai 264209, China * Author to whom correspondence should be addressed; E-Mail: dequn.sun@; Tel.: +86-631-5688537; Fax: +86-631-5688303. Received: 24 May 2011; in revised form: 16 June 2011 / Accepted: 17 June 2011 / Published: 30 June 2011 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. Keywords: pyrimidine derivatives; synthesis; antifungal activity; SAR 1. Introduction Phytopathogenic fungi that easily infect many crops are hard to control and risk resistance to the widely used commercial fungicides [1], therefore, there is a continuous need for new classes of antifungal agents. Natural compounds containing pyrimidine skeletons, such as vitamin B1 [2,3], and nucleotide bases [4] play an important role in life science studies. Pyrimidine derivatives have attracted great interest due to their diverse biological activities. For example, Rashad [5] synthesized a series of 4-hy