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Rapid synthesis of curcuminoid pyrazoles with antiviral effects through one-pot combinatorial modification of total curcuminoids

Authors Wu J, Tang H, Xu J, Ye J, Tian H, Li Y, Jiang R

Received 30 March 2015

Accepted for publication 12 June 2015

Published 3 August 2015 Volume 2015:5 Pages 41—47


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Xing-Cong Li

Jie Wu,1,2 Hong-Jin Tang,1 Jiao-Jiao Xu,1 Juan Ye,3 Hai-Yan Tian,1 Yao-Lan Li,1 Ren-Wang Jiang,1,4

1Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, 2Department of Pharmacy, Renmin Hospital of Wuhan University, 3Department of Pharmacy, Hospital of Huazhong University of Science and Technology, Wuhan, 4Shenzhen Engineering Laboratory of Lingnan Herbal Resource Development and Application, Shenzhen Institute for Drug Control, Shenzhen, People's Republic of China

Abstract: Four new curcuminoid pyrazoles (14) were synthesized by one-pot combinatorial modification of the total curcuminoid extract, through chemical transformation of β-diketone functionalities by p-chlorophenylhydrazine. All four curcuminoid pyrazoles were identified by spectroscopic methods, and the structure of compound 4 was further confirmed by single-crystal X-ray analysis. Compounds 1 and 2, with a long conjugated system and at least one methoxy substitution, showed a more potent antiviral effect than did the corresponding natural product, curcumin. The rapid synthesis of curcuminoid pyrazoles with improved antiviral activity highlights the great potential of one-pot combinatorial modification for the diversification of natural products with improved bioactivities.

Keyword: curcumin, one-pot combinatorial modification, antiviral

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