Citation: Gao Sufan, Zhang Yanchun, Li Jiaming, Zhang Bin, Yang Yu, Hu Mengqi. Synthesis and Biological Evaluation of Novel Phenylpropenoyl-amino Acid Derivatives[J]. Chinese Journal of Organic Chemistry, ;2019, 39(7): 1953-1961. doi: 10.6023/cjoc201812037 shu

Synthesis and Biological Evaluation of Novel Phenylpropenoyl-amino Acid Derivatives

Gao Sufan ^a,b ,
Zhang Yanchun ^a,b ,
Li Jiaming ^a,b,, ,
Zhang Bin ^a,b ,
Yang Yu ^a,b ,
Hu Mengqi ^a,b

a.
College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012
b.
Deparment of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230012

Corresponding author: Li Jiaming, lijiaming2004@sina.com
Received Date: 19 December 2018
Revised Date: 2 February 2019
Available Online: 2 July 2019
Fund Project: Project supported by the National Science and Technology Major Project in 12th Five-Year (No. 2012ZX09401-006)the National Science and Technology Major Project in 12th Five-Year 2012ZX09401-006

Figures(4)

Based on the listed drug rebamipide, a series of novel compounds of phenylpropenoyl-amino acid structures were designed and synthesized according to the pharmacophore-combination strategy. The structures of the target compounds were confirmed by NMR and MS. The inhibitory activities against IL-6 and TNF-α had been investigated. The results demonstrated that all compounds exhibited moderate IL-6 and TNF-α inhibitory activities. In particular, the activities of four compounds were significantly improved than that of rebamipide.
- IL-6,
- TNF-α,
- phenylpropenoyl-amino acid,
- synthesis
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沈阳化工大学材料科学与工程学院沈阳 110142