Preparation of novel 1,2,3-triazole furocoumarin derivatives via click chemistry and their anti-vitiligo activity

Chao Niu; Xueying Lu; Haji Akber Aisa

doi:10.1039/c8ra09755k

Preparation of novel 1,2,3-triazole furocoumarin derivatives via click chemistry and their anti-vitiligo activity

RSC Adv. 2019 Jan 14;9(3):1671-1678. doi: 10.1039/c8ra09755k. eCollection 2019 Jan 9.

Authors

Chao Niu^{1

2}, Xueying Lu^{1

2}, Haji Akber Aisa^{1

2}

Affiliations

¹ Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi 830011 China haji@ms.xjb.ac.cn.
² State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Urumqi 830011 China.

Abstract

The extracts of Psoralea corylifolia L. were often used for the repigmentation of leukoderma (vitiligo) in traditional Uygur medicine thousands years ago. Nowadays, its active ingredient, furocoumarins, has been clinically applied since it exhibited strong photosensitivity. Thus, a new series of furocoumarin derivatives (8a-8o) containing 1,2,3-triazole were designed and synthesized based on our previous work. After biological evaluation for melanin contents and tyrosinase activity in B16 murine cells, the SAR was summarized. The results indicated that five compounds (8a, 8j, 8m-8o) were more potent than the positive control (8-MOP) on melanogenesis. Among them, 8a and 8o showed the best stimulating effect on tyrosinase activity as well, and were submitted for further pharmacological study of anti-vitiligo.