European Journal of Medicinal Chemistry
•Eighteen coumarin derivatives were semisynthesized with potential antiasthmatic properties.•Results indicate that ether derivatives 1–3, 7–9 and 13–15 showed the best relaxant activity.•Compound 2 (42 μM) was the most potent of the entire series, being 4-times more active than theophylline (positive control).
Bioorganic & medicinal chemistry
The last two decades have provided a large weight of preclinical data implicating the neurokinin-1 receptor (NK1) and its cognate ligand substance P (SP) in a broad range of both central and peripheral disease conditions. However, to date, only the NK1 receptor antagonist aprepitant has been approved as a therapeutic and this is to prevent chemothe...
The homomeric α7 nicotinic acetylcholine receptor is a well-studied therapeutic target, though its characteristically rapid desensitization complicates the development of drugs with specific agonist effects. Moreover, some experimental compounds such as GTS-21 (2,4diMeOBA), a derivative of the α7-selective partial agonist benzylidene anabaseine (BA...