Citation:
Bao Lei Wang, Yong Hong Li, Jian Guo Wang, Yi Ma, Zheng Ming Li. Molecular design, synthesis and biological activities of amidines as new ketol-acid reductoisomerase inhibitors[J]. Chinese Chemical Letters,
;2008, 19(6): 651-654.
doi:
10.1016/j.cclet.2008.04.009
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Diamidine (A) was identified in our in vitro bio-assay as a possible inhibitor of ketol-acid reductoisomerase (KARI) from the ACD database search based on the known three-dimensional crystal structure of KARI. An investigation on interaction of A on KARI active sites, led to the design and synthesis of 15 novel monoamidines. Some of those showed better biological activity than A on rice KARI (in vitro) and in greenhouse herbicidal tests (in vivo). The structure-biological activity relationship was investigated, which provides valuable information to further study of potential KARI inhibitors.
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Keywords:
- KARI,
- Molecular design,
- Synthesis,
- Biological activity
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