In vivo metabolism of 2-[1′-phenyl-3′-(3-chlorophenyl)-2′-propenylyden]hydraz ino-3-methyl-4(3H)-quinazolinone in rats

  • Bedıa Koçyıĝıt Kaymakçioĝlu
  • Yasemın Aktan
  • Sıbel Süzen
  • Nesrın Gökhan
  • Semra Koyunoĝlu
  • Kevser Erol
  • Akgül Yeşjxada
  • Sevım Rollas


The aim of this study was to investigate by HPLC the in vivo metabolism of 2-[1′-phenyl-3′-(3-chlorophenyl)-2′-propenylyden]hydrazino-3-methyl-4(3H)-quinazolinone as a substrate, and as a model compound in rats. The substrate was dissolved in DMSO/water (1∶4) and administered intraperitoneally at a dose of 100 mg/kg in a volume of approximately 0.1 mL. Blood samples were taken before and 30 min, 1.5, 3, 6, 9, 11, 30 and 48 h after i.p. drug administration. The chromatographic separation of the substrate and its metabolites was performed using a stainless steel Novopak C18 column (150 × 4.6 mm i.d., 5-μm particle size). The optimal composition of the mobile phase was reached by introducing different mixtures of pure acetonitrile and water in a linear gradient system. Following the biotransformation of this compound, 2-hydrazino-3-methyl-4(3H)-quinazolinone (M1) and 3-(3-chlorophenyl)-1-phenylprop-2-en-1-one (M2) derivatives were identified together with substrate by comparing them to reference standards using HPLC-UV/DAD. In addition, the composition of these metabolites and substrate was confirmed by LC-MS in plasma.


2-[1-phenyl-3-(chlorophenyl)-2-propenylyden]hyarazino-3-methyl-4(3H)-quinazolinone HPLC in vivo metabolism 


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Copyright information

© Springer-Verlag 2005

Authors and Affiliations

  • Bedıa Koçyıĝıt Kaymakçioĝlu
    • 5
  • Yasemın Aktan
    • 1
  • Sıbel Süzen
    • 2
  • Nesrın Gökhan
    • 3
  • Semra Koyunoĝlu
    • 4
  • Kevser Erol
    • 1
  • Akgül Yeşjxada
    • 4
  • Sevım Rollas
    • 5
  1. 1.Department of Pharmacology, Faculty of MedicineOsmangazi UniversityEskişehirTurkey
  2. 2.Department of Pharmaceutical Chemistry, Faculty of PharmacyAnkara UniversityAnkaraTurkey
  3. 3.Department of Pharmaceutical Chemistry, Faculty of PharmacyHacettepe UniversityAnkaraTurkey
  4. 4.Department of Basic Pharmaceutical Sciences, Faculty of PharmacyHacettepe UniversityAnkaraTurkey
  5. 5.Department of Pharmaceutical Chemistry, Faculty of PharmacyMarmara UniversityHaydarpasa, İstanbulTurkey

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