76812-37-8Relevant academic research and scientific papers
UNIQUE DUAL-ACTION THERAPEUTICS
-
Page/Page column 41, (2010/05/14)
A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n = 0, 1; X = C, Si, and N+ and NSAID = ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed
Substituted aminoalcohol ester analogs of indomethacin with reduced toxic effects
Haien, Parmeshwari K.,Chagti, Kewal K.,Giridhar, Rajani,Yadav, Mange Ram
, p. 101 - 111 (2008/04/01)
Synthesis and evaluation of five different N,N-disubstituted aminoethanol ester derivatives of indomethacin bearing structural resemblance to the aminoethanol ester class of anticholinergics are reported herein. The anticholinergic activity was incorporated into the intact esters to overcome the gastric toxicity of indomethacin, not only by blocking the acidic functionality but also by decreasing gastric secretions and motility. These derivatives exhibited in vitro stability in buffers of pH 2.0 and 7.4 for 6 h and were readily hydrolyzed by human plasma esterases to liberate the parent drug. All the derivatives were significantly less irritating to the gastric mucosa than the parent drug. Though only two esters showed antiinflammatory activity similar to that of the parent drug at equivalent dose levels, all the esters were equipotent to indomethacin in the mouse acetic acid-induced writhing assay for analgesic action. The present evaluation indicates that the combined pharmacological properties of these ester derivatives may prove useful for design and development of novel gastric sparing antiinflammatory molecules with potentially important therapeutic applications. Birkhaeuser 2007.
Non Steroidal Antiinflammatory Agents. V. Basic Esters of Indometacin
Kappe, Th.,Fruehwirth, F.
, p. 475 - 478 (2007/10/02)
The reaction of diisopropylcarbodiimid 1a with ethanolamines 2a, b affords isoureas 3a, b which in turn react with indometacin 4 to yield the title compounds 6a, b.The noncatalyzed reaction of 1a, b with 4 (also in the presence of 2) leads to the ureido-indometacines 8a, b.
