It is known that substituted hydrazide hydrazone derivatives have several biological and pharmacological activities; there is limited literature on the metabolism of hydrazide hydrazones in rats. In our previous study, 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene]hydrazide (S) was found active against Staphylococcus aureus ATCC 29213. Therefore, we planned to study the in vivo metabolism of S in rats. The substrate was administered in doses of 50 mg/kg or 100 mg/kg intraperitoneally. Blood samples were collected at 0, 5, 15, 30, 45 min and 1, 1.5, 2, 4, 8, 12, 24, 48 h after administration. The substrate and its potential metabolites were separated using HPLC on a reverse phase system. 4-Fluorobenzoic acid and one unidentified metabolite were detected together with substrate.
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
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