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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