Yu Chen-Sheng, Wang Qiao, Bajsa-Hirschel Joanna, Cantrell Charles L, Duke Stephen O, Liu Xing-Hai
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
U.S. Department of Agriculture, Natural Products Utilization Research Unit, Agricultural Research Service, P.O. Box 1848, University, Mississippi 38677, United States.
J Agric Food Chem. 2021 Jun 16;69(23):6423-6430. doi: 10.1021/acs.jafc.0c07538. Epub 2021 Jun 4.
Nicotinic acid, also known as niacin, is a natural product, which is widely found in plants and animals. To discover novel natural-product-based herbicides, a series of -(arylmethoxy)-2-chloronicotinamides were designed and synthesized. Some of the new -(arylmethoxy)-2-chloronicotinamides exhibited excellent herbicidal activity against (bentgrass) at 100 μM. Compound (2-chloro--((3,4-dichlorobenzyl)oxy)nicotinamide) possessed excellent herbicidal activity against (duckweed), with an IC value of 7.8 μM, whereas the commercial herbicides clomazone and propanil had values of 125 and 2 μM, respectively. The structure-activity relationships reported in this paper could be used for the development of new herbicides against monocotyledonous weeds.
烟酸，又称尼克酸，是一种天然产物，广泛存在于动植物中。为了发现新型基于天然产物的除草剂，设计并合成了一系列α-(芳基甲氧基)-2-氯烟酰胺。一些新型α-(芳基甲氧基)-2-氯烟酰胺在100μM浓度下对匍匐翦股颖表现出优异的除草活性。化合物2-氯-α-((3,4-二氯苄基)氧基)烟酰胺对浮萍具有优异的除草活性，IC50值为7.8μM，而市售除草剂广灭灵和敌稗的IC50值分别为125和2μM。本文报道的构效关系可用于开发针对单子叶杂草的新型除草剂。
