Glycosidase inhibitors: a patent review (2008 – 2013)

Abstract

Introduction: In the recent decades, the interest on glycosidases has dramatically increased, mainly because these enzymes play a key role in many biological processes. The importance of these enzymes is also reflected by a number of diseases, which result from the lack or dysfunction of a given glycosidase, as well as by the use of glycosidase inhibitors in the treatment of metabolic disorders or viral infections. Based on the biological potential associated to these enzymes, several glycosidase inhibitors have been developed. In this review, the most important inhibitors targeting these enzymes, including the disaccharides, iminosugars, carbasugars, thiosugars and other non-glycosidic compounds will be discussed and special attention will be given to the ones that are currently used clinically.

Areas covered: This review summarizes and characterizes the current knowledge regarding the classes of glycosidase inhibitors that have therapeutic potential in a wide range of diseases. It highlights the relevant research, patents and patent applications filed in the past years on the field.

Expert opinion: Since the glycosidase inhibitors are involved in several chronic diseases and possibly pandemic, the pharmaceutical research toward developing new generations of these molecules is very important to public health in the world. The unique combination of these compounds – for example, they share many properties with natural carbohydrates and also possess distinct specific characteristics – makes them precious for pharmaceutical companies in an attempt to search for potential new drugs. Currently, the most promising compounds are the iminosugars and thiosugars due to their better oral bioavailability.

Keywords::

• carbasugars
• catalytic mechanism
• cystic fibrosis
• diabetes
• disaccharides
• Gaucher’s disease
• glucosidases
• glycosidases
• iminosugars
• inhibitors
• non-glycosidic inhibitors
• thiosugars

Acknowledgment

NF Brás and NMFSA Cerqueira have equally contributed to this work.

Notes

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