Evaluation of glycolamide esters of indomethacin as potential cyclooxygenase-2 (COX-2) inhibitors☆

Add time:08/17/2019    Source:sciencedirect.com

A number of novel indomethacin glycolamide esters were synthesized and tested for their cyclooxygenase (COX-1 and COX-2) inhibition properties in vitro. Many of these compounds proved to be selective COX-2 inhibitors, and subtle structural changes in the substituents on the glycolamide ester moiety altered the inhibitory properties as well as potencies significantly. Their in vitro data were rationalized through molecular modeling studies. Few of them displayed anti-inflammatory activity in vivo. Compound 32, [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid 2-morpholin-4-yl-2-oxo ethyl ester, was identified as a promising compound in this class and its good anti-inflammatory activity was demonstrated in the in vivo model.

We also recommend Trading Suppliers and Manufacturers of 2-(2-CHLORO-ACETYLAMINO)-4-P-TOLYL-THIOPHENE-3-CARBOXYLIC ACID ETHYL ESTER (cas 138098-81-4). Pls Click Website Link as below: cas 138098-81-4 suppliers

Prev:Asymmetric chemoenzymatic synthesis of N-acetyl-α-amino esters based on lipase-catalyzed kinetic resolutions through interesterification reactions
Next:Original articleSynthesis and antimicrobial properties of 4-acylaminobenzenethiosulfoacid S-esters)