This work received financial support from the European Union
(FEDER funds POCI/01/0145/FEDER/007265) and National Funds
(FCT/MEC, Fundação para a Ciência e Tecnologia and Ministério da
Educação e Ciência) under the Partnership Agreement PT2020 UID/QUI/50006/2013; FCT UID/QUI/00062/2013, and “Programa Operacional
Competitividade e Internacionalização” (COMPETE) (POCI-
01-0145-FEDER-029241), and under the framework of QREN
(NORTE-01-0145-FEDER-000024). Thanks are also due to Faculdade
de Farmácia da Universidade do Porto and Instituto Politécnico
de Bragança.
α-Glucosidase plays an important role in carbohydrate metabolism and is therefore an attractive therapeutic target for the treatment of diabetes, obesity and other related complications. In the last two decades, considerable interest has been given to natural and synthetic xanthone derivatives in this field of research. Herein, a comprehensive review of the literature on xanthones as inhibitors of α-glucosidase activity, their mechanism of action, experimental procedures and structure-activity relationships have been reviewed for more than 280 analogs. With this overview we intend to motivate and challenge researchers (e.g. chemistry, biology, pharmaceutical and medicinal areas) for the design of novel xanthones as multipotent drugs and exploit the properties of this class of compounds in the management of diabetic complications.
