Synthesis and herbicidal evaluation of novel benzothiazole derivatives as potential inhibitors of D1 protease

被引:5
作者
Huang, Tonghui [1 ,2 ]
Sun, Jie [1 ]
An, Lin [1 ]
Zhang, Lixian [1 ]
Han, Cuiping [3 ]
机构
[1] Xuzhou Med Coll, Sch Pharm, Jiangsu Key Lab New Drug Res & Clin Pharm, Xuzhou 221004, Jiangsu, Peoples R China
[2] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China
[3] Xuzhou Med Coll, Sch Med Imaging, Xuzhou 221004, Jiangsu, Peoples R China
基金
中国国家自然科学基金;
关键词
Benzothiazoles; D1 protease inhibitor; Molecular docking; Herbicidal activities; Synthesis; PHOTOSYSTEM-II; BIOLOGICAL EVALUATION; PROCESSING PROTEASE;
D O I
10.1016/j.bmcl.2016.01.087
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
D1 protease is a C-terminal processing protease that has been predicted to be an ideal herbicidal target. Three novel series of benzothiazole derivatives were synthesized and evaluated for their herbicidal activities against Brassica napus (rape) and Echinochloa crusgalli (barnyard grass). The preliminary bioassay indicated that most of the synthesized compounds possess promising D1 protease inhibitory activities and considerable herbicidal activities. Molecular docking was performed to position representative compounds into the active site of D1 protease to determine a probable binding model. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1854 / 1859
页数:6
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