Synthesis of Some Novel Substituted Benzamides, Their Inhibition of AHAS and Herbicidal Activity

Abstract

Abstract: Based on the strategy of bio-rational design of AHAS inhibitors, 8 novel N-(phenylsulfonamidophenyl)benzamide and 7 novel N-{[N-(phenylsulfonyl)phenylsulfonamido] phenyl}benzamide derivatives were designed and synthesized by starting materials 4-fluoro-3-nitroaniline and 2-amino-5-nitrobenzonitrile, and their structures were confirmed by IR, MS, ¹H NMR and elemental analysis. The preliminary bioassay indicated that some compounds exhibited bioactivity either in vitro or in vivo. Compounds 4c, 4d and 7c show inhibition to Arabidopsis thaliana AHAS of 66%, 76% and 68% at 100 μg/mL. Compound 4a, 4c, 7a and 7b show inhibition on the growth of rape root of 76%, 70%, 89% and 82% at 100 μg/mL. The present results provide helpful guidance to further design more potential AHAS inhibitors.

Key words: Benzamide, AHAS inhibitor, Herbicidal activity

TrendMD:

LI Wen-Ming, WANG Jian-Guo*, LI Yong-Hong, WANG Su-Hua, LI Zheng-Ming*. Synthesis of Some Novel Substituted Benzamides, Their Inhibition of AHAS and Herbicidal Activity[J]. Chem. J. Chinese Universities, 2010, 31(8): 1574.

References

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