期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 14, 期 7, 页码 865-874出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026614666140202204602
关键词
Amine oxidases; drug design; enzyme inhibition; enzyme mechanisms; fluorine; glycosidases; mechanism-based inhibition
资金
- Natural Sciences and Engineering Research Council
- Canadian Institutes for Health Research
- NSERC CREATE
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 alpha-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.
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