69299-58-7Relevant academic research and scientific papers
Synthesis and biological evaluation of ester derivatives of indomethacin as selective COX-2 inhibitors
Babu, M. Arockia,Shukla, Rakesh,Nath, Chandishwar,Kaskhedikar
, p. 2223 - 2228 (2012/11/13)
The ester derivatives of indomethacin were prepared by condensing indomethacin with an equimolar quantity of an appropriate alcoholic compound in anhydrous dichloromethane in the presence of DCC and DMAP. Spectral studies comprising of IR, 1H NMR, mass, and microanalysis were performed in order to confirm their structures. In vivo anti-inflammatory studies were carried out using carrageenan rat paw edema method and in vivo ulcerogenic studies by ulcer index method for the panel of synthesized compounds. Out of eleven compounds, the compound IIc displayed moderate anti-inflammatory activity with no observable ulcerogenic effect when compared to indomethacin. Furthermore, compound IIc, indomethacin and celecoxib were tested at a concentration of 20 μM against COX-1 and COX-2 enzymes by colorimetric COX inhibitor screening assay. Compound IIc was found to be active against COX-2 and COX-1 enzymes exhibiting 62.0 and 12.9% inhibition, respectively. Springer Science+Business Media, LLC 2011.
Synthesis of oligo(ethylene glycol) substituted phosphatidylcholines: Secretory PLA2-targeted precursors of NSAID prodrugs
Rosseto, Renato,Hajdu, Joseph
experimental part, p. 110 - 116 (2010/06/16)
A series of new phosphatidylcholine analogues with structurally modified sn-2-substituents have been prepared. The synthetic compounds include oligo(ethylene glycol) derivatives with chain-terminal pharmacophores that upon catalytic hydrolysis by phospholipase A2 yielded a series of oligo(ethylene glycol)-conjugates of the respective drugs. The approach here outlined may open a new way to employ OEG derivatives of phospholipids for therapeutic applications as secretory PLA2-targeted precursors of prodrugs.
