A series of 1-(2-hydroxyethyl)-3,5-dimethylpyrazolylazo derivatives, incorporating thiosemicarbazide 2a-c, 1,3,4-thiadiazole 3a-c, and 1,2,4-triazole-3-thione 4a-c were synthesized. The structure of these novel synthesized compounds 2a-c, 3a-c, and 4a-c was confirmed by spectral analysis. All these compounds were screened for their analgesic activity. Hot-plate and tail-immersion tests were used for the determination of the analgesic activity. Morphine, an analgesic through both spinal and supraspinal pathways, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg i.p. Among the compounds, 2-(butylamino)-5-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-1,3,4-thiadiazole 3a and 4-[((1-(2-hydroxyethyl)-3,5-dimethylpyrazole-4-yl)azo)phenyl]-4-(2-phenethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 4c showed analgesic effects in both tests. Especially 4c exerted strong analgesia starting at 30 min after injection.

Derivatives (IVa) and (Vc) show analgesic effects in both the hot-plate and tail-immersion tests. Especially the latter exerts strong analgesia starting at 30 min after the injection. -(ORUC, E. E.; KOCYIGIT-KAYMAKCIOGLU, B.; ORAL, B.; ALTUNBAS-TOKLU, H. Z.; KABASAKAL, L.; ROLLAS*, S.; Arch. Pharm. (Weinheim, Ger.) 339 (2006) 5, 267-272; Dep. Pharm. Chem., Fac. Pharm., Marmara Univ., Haydarpasa, TR-81010 Istanbul, Turk.; Eng.) -M. Kowall 35-125

The aim of this study was to investigate absorption of ethyl 2-cyanoacrylate glue when used as a tissue adhesive. Ethyl 2-cyanoacrylate was applied subcutaneously to four rats; its presence in blood and urine was investigated by using High Pressure Liquid Chromatography. Blood samples were drawn at baseline and after 2, 4, 6, 24, 48, 54, 78, 96 hours following application. Urine samples were obtained at baseline and after 4, 24, 48, 72, 96 hours. Administration of ethyl 2-cyanoacrylate resulted in its absorption of unchanged ethyl 2-cyanoacrylate and unknown metabolites, in plasma and urine.

Nimesulide (4-nitro-2-phenoxymethanesulfonanilide) is an atypical NSAID lacking a carboxylic acid moiety. It has a good gastric tolerability due to selective inhibition of COX-2. The study objectives in the present work were to characterize the metabolism of nimesulide in rat plasma at certain time intervals. In vitro studies were also carried out to examine if nitroreduction takes place in vitro using rat hepatic subcellular fractions (microsomal and S9 fraction) besides aromatic hydroxylation. This communication describes detection and characterization of nimesulide metabolites isolated from plasma and hepatic subcellular post-incubates by the use of HPLC-UV/diode array and LC-MS/MS. Hydroxynimesulide was the major metabolite both in vivo and in vitro whereas nitroreduction was observed only in vitro with subcellular fractions under anaerobic conditions.

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