In vivo metabolism of 4-fluorobenzoic acid [(5-nitro-2-furanyl) methylene] hydrazide in rats

Abstract

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.

Thein vivo metabolism of 5-(4-nitrophenyl)-4-(2-phenylethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione in rats

“…Previous results had established that the substrate and its metabolites could be bound to the plasma proteins (8,11). For this reason, the plasma proteins were denatured by heating and blood samples were prepared after the denaturation.…”

“…In this research, the previous methods were used for preparation of blood samples (8,11). Briefly these methods, blood was centrifuged to separated into plasma and blood cells.…”

Absorption of ethyl 2-cyanoacrylate tissue adhesive

“…In this research, the previous methods were used for preparation of blood samples [3,4]. The blood samples were centrifuged and separated into plasma and blood cells.…”

The synthesis and biological activities of 3-acyl- 2,3-dihydro-1,3,4-oxadiazole/ 3-acyl-1,3,4-oxadiazoline derivatives obtained from hydrazide-hydrazones

“…The acyl-and aroylhydrazones are very important as chelating agents (11)(12)(13)(14) Compounds containing hydrazide and hydrazone moiety proved to be especially attractive due to their application in biology (4,(15)(16)(17)(18)(19)(20)(21) and medicine, isocarboxazide, iproniazide, isoniazid, nifuroxazide, rifampisin as example drugs. Also hydrazones are the most important compounds for prodrug design due to their poor metabolic stability (1,(22)(23)(24). The plasma stability of the prodrugs is very important for rapid conversion in plasma (25).…”

“…The substituted 1,3,4-oxadiazole derivatives have been obtained from hydrazide-hydrazones by the oxidative cyclization (35)(36)(37). The hydrazone functional group is usually not stable in vivo (22,38) and in vitro (23,39). However the hydrolytic stability of hydrazones are depend on the structure of the substituent (1).…”