Volume 33, Issue 4 pp. 486-494
Full Paper

Synthesis and Bioactivity of New Chalcone Derivatives as Potential Tyrosinase Activator Based on the Click Chemistry

Chao Niu

Chao Niu

Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

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Gen Li

Gen Li

Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

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Adila Tuerxuntayi

Adila Tuerxuntayi

Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

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Haji A. Aisa

Corresponding Author

Haji A. Aisa

Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, China

Key Laboratory of Plant Resources and Chemistry of Arid Zone, Chinese Academy of Sciences, Urumqi, Xinjiang 830011, ChinaSearch for more papers by this author
First published: 30 March 2015
Citations: 20

Abstract

A new series of (E)-1-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-3-phenylprop-2-en-1-one 1a(4-((1-benzyl-1H-1,2,3-triazol-4-yl) methoxy)phenyl)-1-phenylprop-2-en-1-one 1b15b were designed, synthesized based on click chemistry, and biologically evaluated for their activity on tyrosinase. The result showed that most of prepared compounds 1a15a have potent activating effect on tyrosinase, especially for 3a, 8a10a and 14a15a. Among them, compounds 10a and 14a demonstrated the best activity with EC50=1.71 and 5.60 µmol·L−1 respectively, even better than the positive control 8-MOP (EC50=14.8 µmol·L−1). Conversely, compounds 3b, 5b6b, 9b10b, and 15b induced enzymatic inhibition on tyrosinase.

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