Discovery of potent CRTh2 (DP2) receptor antagonists
摘要:
Starting with the weak agonist indomethacin, a series of potent, selective CRTh2 (DP2) antagonists have been discovered as potential treatments for asthma, allergic rhinitis and other inflammatory diseases. (c) 2006 Elsevier Ltd. All rights reserved.
作者:Parul Pal、Meghan Fragis、Jakob Magolan、Srinivas Dharavath、Jarrod W. Johnson
DOI:10.1055/a-1868-4148
日期:2022.11
Fischer indole reactions. These vinyl sulfides react with arylhydrazines in the presence of TsOH·H2O in refluxing ethanol or dichloroethane to yield diverse 3-substituted and 2,3-disubstituted indoles or azaindoles. The utility of this chemistry is highlighted with the efficient preparation of three biomedically relevant compounds: 4-aza-melatonin, a furoindoline, and an indomethacin-like CRTh2 antagonist