Evaluation of glycolamide esters of indomethacin as potential cyclooxygenase-2 (COX-2) inhibitors |
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Authors: | Khanna Smriti Madan Manjula Vangoori Akhila Banerjee Rahul Thaimattam Ram Jafar Sadik Basha S K Ramesh Mullangi Casturi Seshagiri Rao Pal Manojit |
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Institution: | Department of Chemistry, Discovery Research, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500049, India. |
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Abstract: | 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. |
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