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Progress in the Development of Platelet‐Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases

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Hyland, IKP ORCID: 0000-0001-9850-0238, O'Toole, RF ORCID: 0000-0002-4579-4479, Smith, JA ORCID: 0000-0001-6313-3298 and Bissember, AC ORCID: 0000-0001-5515-2878 2018 , 'Progress in the Development of Platelet‐Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases' , ChemMedChem , doi: 10.1002/cmdc.201800401.

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Abstract

Platelet-activating factor (PAF) and its receptor (PAFr) have been implicated in a wide range of diseases and disorders that originate from the activation of inflammatory pathways. Although the exact structure of the binding site on the PAFr remains unknown, the PAFr is a well-established therapeutic target, and an array of structurally diverse PAFr antagonists have been identified. These include compounds that are structurally similar to the natural PAF ligand, synthetic heterocycles, complex polycyclic natural products, and various metal complexes. This review provides an update on more than 20 years of progress in this area. The development and synthesis of new PAFr antagonists, structure-activity relationship studies, the biological activity of these molecules, and their therapeutic potential are discussed.

Item Type: Article
Authors/Creators:Hyland, IKP and O'Toole, RF and Smith, JA and Bissember, AC
Keywords: ginkgolides, inflammatory diseases, platelet-activating factor, thienodiazepines, xanthones
Journal or Publication Title: ChemMedChem
Publisher: Wiley-VCH
ISSN: 1860-7179
DOI / ID Number: 10.1002/cmdc.201800401
Copyright Information:

Copyright 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

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