Evaluation of anti-inflammatory and analgesic activities of some newly synthesized pyrazole derivatives
Souraya Domiati, Ahmed El-Mallah, Asser Ghoneim, Adnan Bekhit and Heba Abd El Razik
Beirut Arab University, Lebanon
Pharos University, Egypt
Damanhur University, Egypt
Alexandria University, Egypt
: J Pharm Drug Deliv
Abstract
NSAIDs are associated with several side effects such as gastrointestinal mucosal damage, renal toxicity and cardiovascular side effects. Aiming to find a novel analgesic/anti-inflammatory drug with minimal side effects, the present study was designed to screen and evaluate some newly synthesized pyrazole derivatives. Anti-inflammatory activity, COX-1/COX-2 selectivity, analgesic as well as ulcerogenic and renal side effects of the compounds were assessed. The results of the carrageenan-induced rat paw edema showed that the carboxyphenylhydrazone derivative, was more potent than the chlorophenyl counterpart with a relative activity compared to celecoxib of 1.08 and -0.13, respectively after 1 hour. Moreover, the carboxyphenylhydrazone derivative had good analgesic activity but caused significant increase in the ulcer index, creatinine and BUN levels.The cotton granuloma test showed that cyano derivatives of pyrazole have good anti-inflammatory activity. Adding an acetyl group on C28H12N6SO2 not only increased the anti-inflammatory activity from a relative activity compared to celecoxib of 0.57 to 1.17 in the granuloma test, but also increased the selectivity toward COX-2 from 0.197 to 47.979. As a conclusion, from the ten compounds analyzed, three compounds showed to be the most effective ones as analgesic/ anti-inflammatory agents with low ulcerogenicity and nephrotoxicity.
Biography
Email: t.domyati@bau.edu.lb
