Synthesis of novel naphthalene COX inhibitors for anti-inflammatory activity

Abstract

Inflammation forms the part of various diseased conditions. To treat inflammation variety of anti inflammatory agents are synthesized, they showed undesirable side effects. In order to avoid these side effects, nonsteroidal anti-inflammatory drugs were developed. Research is a continuous and never ending process; efforts are being made to improve the present drug profile such that present side effects can be eliminated. Syntheses of number of naphthalene derivatives with pyrazole moiety were completed. The present classification records for numerous naphthalene derivatives (naproxen and nabumetone) and also many anti-inflammatory drugs containing diaryl heterocycle(celecoxib,rofecoxib) are available as reference, therefore some new non-vicinal 3,5 diaryl heterocycles,in which naphthalene as one of aryl ring and pyrazole as central scaffold was prepared and evaluated for anti-inflammatory activity. The purity of all compounds has been examined by the TLC and structure is confirmed by different analytical techniques like IR, Mass spectroscopy and NMR. Further, the synthesized drugs were evaluated for in vivo anti inflammatory activity by carrageenan induced rat paw edema test using Indomethacin as a standard drug. In conclusion, we have found that two compounds showed equipotent activity while other two showed slightly more anti-inflammatory activity respectively.