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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.

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