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Design, synthesis and herbicidal activities of novel 4‐(1 H ‐pyrazol‐1‐yl)‐6‐(alkynyloxy)‐pyrimidine derivatives as potential pigment biosynthesis inhibitors
Author(s) -
Ma HongJu,
Zhang JianHua,
Xia XiangDong,
Xu MengHan,
Ning Jun,
Li JianHong
Publication year - 2014
Publication title -
pest management science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.296
H-Index - 125
eISSN - 1526-4998
pISSN - 1526-498X
DOI - 10.1002/ps.3633
Subject(s) - brassica , pyrimidine , pyrazole , pigment , biosynthesis , chemistry , biological pigment , pennisetum , in vivo , ic50 , biochemistry , in vitro , biology , stereochemistry , botany , organic chemistry , enzyme , microbiology and biotechnology
BACKGROUND With the objective of finding novel valuable herbicidal candidates, a series of novel 4‐(1 H ‐pyrazol‐1‐yl)‐6‐(alkynyloxy)‐pyrimidine derivatives were synthesised and their herbicide activities were evaluated in vivo . RESULTS The results showed that many target compounds expressed bleaching activities. Among these, compound 5 h showed the best bleaching activity to gramineous weeds, being able to produce the highest inhibition of chlorophyll level in seedlings of Pennisetum alopecuroides L. ( IC 50 = 3.48 mg L −1 ). Moreover, compound 5 h expressed good selective toxicity between gramineous P. alopecuroides L. and broadleaf plant Brassica campestris L . CONCLUSIONS The present work demonstrates that pyrimidine derivatives containing pyrazole can be used as potential lead compounds for developing novel pigment biosynthesis inhibitors. © 2013 Society of Chemical Industry