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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 KARl.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.
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 KAR1. 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). structure-biological activity relationship was investigated, which provides valuable information to further study of potential KARI inhibitors.