期刊论文

Xi Zhen

英文

Bioorganic & Medicinal Chemistry

0968-0896

2013

21

11

3245-3255

10.1016/j.bmc.2013.03.056

We thank Dr. Jie Chen for the greenhouse testing of biological activities. The research was supported in part by the National Basic Research Program of China (No. 2010CB126103 ), the NSFC (No. 21002038 , 20902034 , and 20925206 ), and the National Key Technologies R&D Program ( 2011BAE06B05 ).

本校为第一机构

Protoporphyrinogen oxidase (PPO, E.C. 1.3.3.4) is the action target for several structurally diverse herbicides. A series of novel 4-(difluoromethyl)-1- (6-halo-2-substituted-benzothiazol-5-yl)-3-methyl-1H-1,2,4-triazol-5(4H)-ones 2a-z were designed and synthesized via the ring-closure of two ortho-substituents. The in vitro bioassay results indicated that the 26 newly synthesized compounds exhibited good PPO inhibition effects with Ki values ranging from 0.06 to 17.79 μM. Compound 2e, ethyl 2-{[5-(4- (difluoromethyl)-3-methyl-5-oxo-4,5-dihydr...