Affiliation:
1. College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China
2. CQM - Centro de Quimica da Madeira, Universidade da Madeira, Campus da Penteada, 9000-390 Funchal, Portugal
3. School of Pharmacy, Nanjing Medical University, Nanjing 211166, China
Abstract
α-Glucosidase plays an important role in carbohydrate metabolism and is an attractive drug
target for the treatment of diabetes, obesity and other related complications. Currently, acarbose, miglitol
and voglibose have been approved by the FDA for the treatment of diabetes by oral α-glucosidase inhibitors.
With the development of anti-diabetic drugs, the emergence of novel drugs with various chemotypes
has overshadowed α-glucosidase inhibitors. Since the 1990s, the FDA has not approved new chemical
entities against α-glucosidase, which has resulted in restricted clinical medication. Nevertheless,
this type of inhibitors possess several unparalleled advantages over other drugs, especially mild side
effects (non-systemic gastrointestinal side effects and occasional allergic reactions). Additionally,
α-glucosidase inhibitors for monotherapy or in combination with other drugs have been proved to be a
feasible approach for the treatment of diabetes. In the last decade, the discovery of natural or synthetic
indole derivatives possessing the inhibitory activity of α-glucosidase has received great attention.
Herein, we have summarized indoles as inhibitors of α-glucosidase activity, their mechanism of action,
synthetic methodologies and structure-activity relationships. Moreover, we have compared the inhibitory
potencies of all compounds under their corresponding positive control as well as oral absorption
in silico evaluated by tPSA. This review will provide a medium on which future drug design and development
for the treatment of diabetes may be modeled as many drug candidates with present great
potential as effective anti-diabetic chemotherapy.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology,General Medicine
Cited by
18 articles.
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