Molecular design, synthesis and biological activities of amidines as new ketol-acid reductoisomerase inhibitors |
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Authors: | Bao Lei Wang Yong Hong Li Jian Guo Wang Yi Ma Zheng Ming Li |
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Affiliation: | Elemento-Organic Chemistry Institute, State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China |
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Abstract: | 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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