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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Fluorinated Mechanism-Based Inhibitors: Common Themes and Recent Developments

Author(s): Christina Tysoe and Stephen G. Withers

Volume 14, Issue 7, 2014

Page: [865 - 874] Pages: 10

DOI: 10.2174/1568026614666140202204602

Price: $65

Abstract

Mechanism-based inhibitors are relatively chemically inert compounds that become activated when processed by their target enzyme, leading to covalent enzyme inactivation. Fluorine substitution confers a number of properties that are beneficial to the chemistry of such inhibitors and to their potential use as pharmaceuticals, and indeed several fluorinated mechanism-based inhibitors have made it to clinical usage over the past 50 years. Well-known examples are the 5- fluorouracil metabolite, 5-fluoro-2’-deoxyuridine-5’-monophosphate, which is used in the treatment of cancer, and α- difluoromethylornithine for the treatment of African sleeping sickness. As the prevalence of fluorine in medicinal chemistry continues to rise, more and more medically relevant fluorinated mechanism-based inhibitors are being developed with a variety of interesting properties and uses.

Keywords: Amine oxidases, drug design, enzyme inhibition, enzyme mechanisms, fluorine, glycosidases, mechanism-based inhibition.

Graphical Abstract

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