Chemical exploration of 4-(4-fluorobenzyl)piperidine fragment for the development of new tyrosinase inhibitors

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• 作者：Stefania Ferro^a ; ^{sferro@unime.it} ; Laura De Luca^a ; Maria Paola Germanò ; ^a ; Maria Rosa Buemi^a ; Laura Ielo^a ; Giovanna Certo^a ; ^b ; Margarita Kanteev^c ; Ayelet Fishman^c ; Antonio Rapisarda^a ; Rosaria Gitto^a
• 关键词：Synthesis ; Tyrosinase inhibitors ; SARs ; Kinetic mechanism ; Docking studies ; Crystallography
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：992-1001
• 全文大小：1274 K
• 卷排序：125

文摘

New indole derivatives as mushroom tyrosinase inhibitors were designed and synthesized. Biochemical assays demonstrated that several obtained compounds proved to be effective tyrosinase inhibitors. For the selected compounds the inhibition kinetics were analyzed by Lineweaver–Burk plots. Docking studies and X-ray co-crystal structure analysis helped us to clarify the binding mode of the most active derivative.