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《中国化学会第十四届全国有机合成化学学术研讨会会议论文集》2017年
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Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as potential AHAS inhibitors

Zi-Li Ren  Wei Wang  Hao Liu  Hao-Tian Hu  Quan-Wei Ma  Xian-Hai Lv  
【摘要】:Acetohydroxy acid synthase(AHAS;EC 2.2.1.6,also referred to as acetolactate synthase,ALS)has been considered as an attractive target for the design of herbicides~([1]).In this work,an optimized pyrazole sulfonamide base scaffold was designed and introduced to derive novel potential AHAS inhibitors by introducing a pyrazole ring in flucarbazone.~([2])The results of in vivo herbicidal activity evaluation indicates compound 3b has the most potent activity with rape root length inhibition values of 81%at 100mg/L,and exhibited the best inhibitory ability against Arabidopsis thaliana AHAS.With molecular docking,compound 3b insert into Arabidopsis thaliana AHAS stably by an H-bond with Arg 377 and cation–πinteractions with Arg 377,Trp 574,Tyr 579.This study suggests that compound 3b may serve as a potential AHAS inhibitor which can be used as a novel herbicides and provides valuable clues for the further design and optimization of AHAS inhibitors.

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