Synthesis of Isatin Derivatives and Their Inhibition Against AHAS

Chem. J. Chinese Universities

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Synthesis of Isatin Derivatives and Their Inhibition Against AHAS

TAN Hai-Zhong, LI Hui-Dong, WANG Jian-Guo*, LI Wen-Ming, LI Yong-Hong, LI Zheng-Ming^*

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

Received:2008-06-05 Revised:1900-01-01 Online:2009-03-10 Published:2009-03-10
Contact: WANG Jian-Guo, LI Zheng-Ming

Abstract

Abstract: Based on the crystal structure of AHAS enzyme, bio-rational drug design was used to discover some novel AHAS inhibitors via computational virtual screening. Some isatin derivatives as AHAS inhibitors were designed, synthesized and evaluated. The preliminary results show that the isatin compounds exhibit conside-rate inhibition both in vivo and in vitro against AHAS. Compound 13 show an inhibition of 85% at 100 μg/mL concentration in vitro and compound 7 show an inhibition of 84.7% of rape root length at 100 μg/mL concentration. This discovery provides meaningful information for further design and synthesis of novel compounds with enhanced activity.

Key words: Novel AHAS inhibitor, Isatin derivatives, Biological activity

CLC Number:

O626

TrendMD:

TAN Hai-Zhong, LI Hui-Dong, WANG Jian-Guo*, LI Wen-Ming, LI Yong-Hong, LI Zheng-Ming^*. Synthesis of Isatin Derivatives and Their Inhibition Against AHAS[J]. Chem. J. Chinese Universities, doi: .

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Synthesis of Isatin Derivatives and Their Inhibition Against AHAS

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