3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 3: Synthesis, metabolic stability, and biological evaluation of optically active analogs

Add time:09/02/2019    Source:sciencedirect.com

A series of 3-(2-aminocarbonylphenyl)propanoic acid analogs possessing the (1R)-1-(3,5-dimethylphenyl)-3-methylbutylamine moiety on the carboxyamide side chain were synthesized and evaluated for their binding affinity for the EP1-4 receptors and their antagonist activity for the EP3 receptor. Rational drug design based on the structure of the metabolites in human liver microsomes led us to the discovery of another series of analogs. Several compounds were further evaluated for their in vivo efficacy in rats after oral administration and also for their pharmacokinetic profiles including in vitro stability in the liver microsomes.

We also recommend Trading Suppliers and Manufacturers of Propanoic acid, 3-(3-chlorophenoxy)-, Methyl ester (cas 18442-28-9). Pls Click Website Link as below: cas 18442-28-9 suppliers

Prev:Short communicationCapillary liquid chromatography of chlorophenoxy acid herbicides and their esters in apple juice samples after preconcentration on a cation exchanger based on polydivinylbenzene-N-vinylpyrrolidone
Next:Identifying dominant conformations of N-acetyl-l-cysteine methyl ester and N-acetyl-l-cysteine in water: VCD signatures of the amide I and the CO stretching bands)