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 shu

Molecular design, synthesis and biological activities of amidines as new ketol-acid reductoisomerase inhibitors

Elemento-Organic Chemistry Institute, State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China

Received Date: 10 December 2007

Fund Project: This work has been kindly supported by the National Basic Research Program of China (No. 2003CB114406) and Specialized Research Fund for the Doctoral Program of Higher Education (No. 20070055044). We thank Dr. R.G. Duggleby of Queensland University (Australia) for his invaluable discussion and technical assistance.

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.
- KARI,
- Molecular design,
- Synthesis,
- Biological activity
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