High-pressure liquid chromatographic analysis for identification of in vitro and in vivo metabolites of 4-phenethyl-5-[4-(1-(2-hydroxyethyl)-3,5-dimethyl-4-pyrazolylazo)phenyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione in rats

Kaymakçıoğlu, Bedia Koçyiğit; Oruç, E. E.; Ünsalan, Seda; Kabasakal, Levent; Rollas, Sevım

doi:10.1016/j.jchromb.2005.12.001

Cited by 6 publications

(3 citation statements)

References 24 publications

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“…Plasma samples were prepared by precipitating plasma proteins with acetonitrile-methanol (50:50 v/v). The advantage of this study procedure was the precipitation of proteins without an extraction step such as liquid-liquid extraction or solid phase extraction (20).…”

Section: Resultsmentioning

confidence: 99%

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High pressure liquid chromatographic analysis ofin vivo metabolites ofN(substituted phenyl)-N′-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats

Koçyığıt‐Kaymakcioğlu

Yılmaz

Arıcıoğlu

2007

Eur. J. Drug Metabol. Pharmacokinet.

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The aim of this study was to investigate the in vivo metabolism of N-(substituted phenyl)-N'-(1,3,5-trimethylpyrazole-4-yl)thioureas (substrate) as model compounds in rats via HPLC. The substrates, N-(4-fluoro/chlorophenyl)-N'-(1,3,5-trimethylpyrazole-4-yl)thioureas (T2 and T3), and their possible metabolites were synthesized and the structures of the compounds were elucidated both by spectral and elemental analysis. Substrates were dissolved in 5% gum arabic and administered 100 mg/kg intraperitoneally (i.p.) in a volume of 0.1 ml/100 g. Blood samples were withdrawn before and at 30 min, 1, 2, 4, 8, 12 and 24 h post-dose. Chromatographic separation of the substrate and its metabolites was performed using a Hichrom chromasil C18 column (150 mm x 4.6 mm i.d., 5 microm particle size). The optimal composition of the mobile phase was achieved by using different mixtures of pure methanol and water. From the biotransformation of these thiourea compounds, N-dealkylation metabolites N-(4-fluoro/chloro-phenyl)-N'-(3,5-dimethylpyrazole-4-yl)thioureas (TI and T4) were identified together with unchanged substrate (T2 and T3) in the plasma by comparing them to reference standards via HPLC UV/DAD.

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Section: Resultsmentioning

confidence: 99%

“…Plasma specimens were treated according to a previously reported method [20]. Cold acetonitrile-methanol (50:50 v/v) (1 ml) mixture was added to 100 III plasma to precipitate plasma proteins, and centrifuged at 10,000 rpm for 10 min.…”

Section: Animals Collection Of Blood Samples and Preparation Of Plasmentioning

confidence: 99%

High pressure liquid chromatographic analysis ofin vivo metabolites ofN(substituted phenyl)-N′-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats

Koçyığıt‐Kaymakcioğlu

Yılmaz

Arıcıoğlu

2007

Eur. J. Drug Metabol. Pharmacokinet.

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“…[10][11][12][13] Hydrazone dyes are considered non-genotoxic and non-mutagenic; e.g., 2-[(2-methoxy-5-nitrophenyl)hydrazono]-N-(2-methoxyphenyl)-3-oxobutanamide (PY74) is a hydrazone pigment used in yellow tattoo inks. The metabolism of PY74 14 and compounds containing azo group 15,16 has been investigated using rat liver and human liver microsomes.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and elucidation of structure of hydrazones derived from N-(2,4-dimethylphenyl)-3-oxobutanamide

Hamzaçebi¹,

Rollas²,

Küçükgüzel³

et al. 2008

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In VivoMetabolism in Preclinical Drug Development

Rollas

2010

Pharmaceutical Sciences Encyclopedia

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In preclinical drug discovery, investigation of the in vitro, in vivo metabolism and toxicity screening of a drug candidate together play a very important role in the drug's success before entering into clinical use. Several in vitro models, such as isolated perfused livers, liver tissue slices, freshly isolated hepatocytes in suspension, primary hepatocyte cultures, cell lines, microsomes, mitochondria, and expression systems have been developed to profile human metabolism. This article focuses on the preclinical in vivo metabolism of drug candidates and prodrugs.

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High-pressure liquid chromatographic analysis for identification of in vitro and in vivo metabolites of 4-phenethyl-5-[4-(1-(2-hydroxyethyl)-3,5-dimethyl-4-pyrazolylazo)phenyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione in rats

Cited by 6 publications

References 24 publications

High pressure liquid chromatographic analysis ofin vivo metabolites ofN(substituted phenyl)-N′-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats

High pressure liquid chromatographic analysis ofin vivo metabolites ofN(substituted phenyl)-N′-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats

Synthesis and elucidation of structure of hydrazones derived from N-(2,4-dimethylphenyl)-3-oxobutanamide

In VivoMetabolism in Preclinical Drug Development

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