Selective glycosidase inhibitors: A patent review (2012-present)

Int J Biol Macromol. 2018 May:111:82-91. doi: 10.1016/j.ijbiomac.2017.12.148. Epub 2018 Jan 2.

Abstract

In the recent decades, the interest on glycosidases has dramatically increased, mainly because these enzymes play a vital role in many biological processes. 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, monocyclic iminosugars, bicyclic iminosugars, thiosugars and carbasugars will be discussed and special attention will be given to the ones that are currently used clinically. 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 patents, relevant research and patent applications filed in the past years in the field. Since the glycosidase inhibitors are involved in several chronic diseases and possibly pandemic, the pharmaceutical research towards developing new generations of these molecules is very important to public health. Most of the glycosidase inhibitors mimics the structures of monosaccharides or oligosaccharides and are well accepted by the organisms since they benefit from privileged drug-like properties. Disaccharides, iminosugars, carbasugars and thiosugars derivatives are the most popular inhibitors among the glycosidase inhibitors.

Keywords: Carbasugars; Disaccharides; Glucosidases; Glycosidases; Iminosugars; Thiosugars.

Publication types

  • Review

MeSH terms

  • Carbasugars / chemistry
  • Carbasugars / therapeutic use
  • Disaccharides / chemistry*
  • Disaccharides / therapeutic use
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / therapeutic use
  • Glycoside Hydrolases / antagonists & inhibitors
  • Glycoside Hydrolases / chemistry*
  • Humans
  • Imino Sugars / chemistry*
  • Imino Sugars / therapeutic use
  • Thiosugars / chemistry
  • Thiosugars / therapeutic use

Substances

  • Carbasugars
  • Disaccharides
  • Enzyme Inhibitors
  • Imino Sugars
  • Thiosugars
  • Glycoside Hydrolases