Design, Synthesis, and in Vitro Evaluation of 4‐(4‐Hydroxyphenyl)piperazine‐Based Compounds Targeting Tyrosinase
2022; Wiley; Volume: 17; Issue: 21 Linguagem: Inglês
10.1002/cmdc.202200305
ISSN1860-7187
AutoresSalvatore Mirabile, Maria Paola Germanò, Antonella Fais, Lisa Lombardo, Federico Ricci, Sonia Floris, Anna Cacciola, Antonio Rapisarda, Rosaria Gitto, Laura De Luca,
Tópico(s)Phytochemicals and Antioxidant Activities
ResumoMelanin biosynthesis is enzymatically regulated by tyrosinase (TYR, EC 1.14.18.1), which is efficiently inhibited by natural and synthetic phenols, demonstrating potential therapeutic application for the treatment of several human diseases. Herein we report the inhibitory effects of a series of (4-(4-hydroxyphenyl)piperazin-1-yl)arylmethanone derivatives, that were designed, synthesised and assayed against TYR from Agaricus bisporus (AbTYR). The best inhibitory activity was predominantly found for compounds bearing selected hydrophobic ortho-substituents on the aroyl moiety (IC
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