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Synthesis, antifungal activity and CoMFA analysis of novel 1,2,4-triazolo[1,5-a]pyrimidine derivatives

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成果类型:
期刊论文
作者:
Chen, Qiong;Zhu, Xiao-Lei;Jiang, Li-Li;Liu, Zu-Ming;Yang, Guang-Fu*杨光富
通讯作者:
Yang, Guang-Fu
作者机构:
[Yang, Guang-Fu; Zhu, Xiao-Lei; Liu, Zu-Ming; Jiang, Li-Li; Chen, Qiong] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Yang, Guang-Fu] C
Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
语种:
英文
关键词:
1,2,4-Triazolo[1,5-a]pyrimidine;1,3,4-Oxadiazole;Antifungal activity;CoMFA
期刊:
European Journal of Medicinal Chemistry
ISSN:
0223-5234
年:
2008
卷:
43
期:
3
页码:
595-603
基金类别:
The present work was supported by National “973” Project (2003CB114400), National NSFC (Nos. 20572030, 20528201, and 20432010), Key project of Ministry of Education (Nos. 103116 and 104205), and Program for Excellent Research Group of Hubei Province (No. 2004ABC002).
机构署名:
本校为第一且通讯机构
院系归属:
化学学院
摘要:
In order to search novel agrochemicals with higher antifungal activity, a series of new 1,2,4-triazolo[1,5-a]pyrimidine derivatives bearing 1,3,4-oxadiazole moieties were designed and synthesized. Their antifungal activities against Rhizoctonia solani were evaluated in vitro. By determining the EC50 values of all the newly synthesized compounds and 10 formerly synthesized compounds, compound 8r, 2-((5-(sec-butylthio)-1,3,4-oxadiazol-2-yl)-methylthio)-5-dimethyl-1,2,4-triazolo-[1,5-a]pyrimidine, was found to display the highest antifungal activi...

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