Armer Richard E, Ashton Mark R, Boyd Edward A, Brennan Chris J, Brookfield Frederick A, Gazi Lucien, Gyles Shân L, Hay Philip A, Hunter Michael G, Middlemiss David, Whittaker Mark, Xue Luzheng, Pettipher Roy
Oxagen Ltd., 91 Milton Park, Abingdon, Oxfordshire, OX14 4RY, UK.
J Med Chem. 2005 Oct 6;48(20):6174-7. doi: 10.1021/jm050519b.
Prostaglandin D2 (PGD2) acting at the CRTH2 receptor (chemoattractant receptor-homologous molecule expressed on Th2 cells) has been linked with a variety of allergic and other inflammatory diseases. We describe a family of indole-1-sulfonyl-3-acetic acids that are potent and selective CRTH2 antagonists that possess good oral bioavailability. The compounds may serve as novel starting points for the development of treatments of inflammatory disease such as asthma, allergic rhinitis, and atopic dermatitis.
作用于CRTH2受体（Th2细胞上表达的趋化因子受体同源分子）的前列腺素D2（PGD2）与多种过敏性疾病及其他炎症性疾病相关。我们描述了一类吲哚-1-磺酰基-3-乙酸，它们是强效且选择性的CRTH2拮抗剂，具有良好的口服生物利用度。这些化合物可作为开发治疗哮喘、过敏性鼻炎和特应性皮炎等炎症性疾病药物的新起点。
Zotero 插件