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

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Progress in the Development of Platelet‐Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases
ChemMedChem ( IF 3.6 ) Pub Date : 2018-08-16 , DOI: 10.1002/cmdc.201800401
Isabel K. Hyland ₁ , Ronan F. O'Toole ₂ , Jason A. Smith ₁ , Alex C. Bissember ₁

Affiliation

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.

中文翻译：

血小板活化因子受体（PAFr）拮抗剂的开发进展及其在炎性疾病治疗中的应用

血小板激活因子（PAF）及其受体（PAFr）已与多种由炎症途径激活引起的疾病和失调有关。尽管尚不清楚PAFr上结合位点的确切结构，但PAFr是已确立的治疗靶标，并且已鉴定出一系列结构多样的PAFr拮抗剂。这些化合物包括在结构上类似于天然PAF配体的化合物，合成杂环，复杂的多环天然产物以及各种金属络合物。这篇综述提供了该领域20多年的最新进展。讨论了新型PAFr拮抗剂的开发与合成，结构-活性关系研究，这些分子的生物学活性及其治疗潜力。

更新日期：2018-08-16

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