Evaluation of analgesic anti inflammatory Anti ulcer and anti bacterial activity of Indazole and its derivatives

Abstract

The earlier studies reveal the various biological activities of the heterocyclic newlinecompound of indazole moiety derivatives, including anti-inflammatory, newlineantimicrobial, anti-HIV, anticancer, hypoglycemic, antiprotozoal, antihypertensive, newlineand other activities. From the observed biological activities of the indazole moiety, newlinethis is concluded that the medicinal properties of indazole have to be explored in the newlinenear future for the treatment of various physiological and pathological conditions. newlineNon-steroidal anti-inflammatory drugs (NSAIDs) are the most widely used newlinemedications in the world; 300 million people worldwide are estimated to use newlineNSAIDs. The pharmacological activity of these agents is related to the suppression newlineof prostaglandin biosynthesis from arachidonic acid by inhibiting the activity of the newlineenzyme cyclooxygenases (COX-1 and COX-2). Therefore chronic use of these nonselective newlineagents may elicit appreciable gastrointestinal ulceration and bleeding. The newlineincidence of clinically significant GI side effects due to NSAIDs is high (over 30%) newlineand causes some patients to abandon NSAID therapy. The present study tested newlinecompounds was designed to investigate the pharmacological actions of analgesic, newlineanti-inflammatory, anti-ulcer and anti-bacterial activity of indazole, 5 newlineaminoindazole and 6 nitroindazole. The anti-nociceptive effect was studied using newlinethree different nociceptive assays and possible mechanisms through appropriate newlineinteracting agents. The carrageenan induced rat paw edema was employed for newlineanti- inflammatory activity and further investigate the possible cellular mechanisms newlineunderlying the anti-inflammatory effect, aspirin induced method for gastric ulcer newlineprotection, agar well diffusion for anti-bacterial activity. The present study newlineidentified that anti - nociceptive and anti-inflammatory activity was observed in all newlinetested compounds and maximum effect was observed in 5-aminoindazole. Indazole newlineand its derivatives significantly, dose dependently and time dependently inhibited newlinecarrageenan induced hind paw oedema. In addition, the test compounds inhibited newlinecyclooxygenase 1 and 2, pro-inflammatory cytokines and free radicals in a newlineconcentration dependent manner and inhibitory activity of COX-2 was higher than the newlineCOX-1 in all tested compounds. It was a l s o observed that, all tested compounds newlinewere ulcer protective against NSAIDS; they may be used alone or in addition, they newlinecan be combined with any of the currently used NSAID to improve its therapeutic newlineefficacy and at the same time to blunt /offset gastric ulceration, the most feared newlineadverse effect of NSAID. And also anti-bacterial activity was observed in newlinesubstituted indazoles like 5-aminoindazole, and 6-nitroindazole in the present study newlinewhich is useful in some bacterial infections associated with pain and inflammatory newlineconditions. SPSS 16 was utilized for Statistical analysis. ANOVA, Dunnet t test newlineand Paired t test were used to analyse the data obtained from various newlineexperiments. A probability value less than 5% was considered to be statistically newlinesignificant. newline newline newline