Kaymakcioğlu Bedia Koçyiğit, Rollas Sevim, Kartal-Aricioğlu Feyza
Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpasa, Istanbul, Turkey.
Eur J Drug Metab Pharmacokinet. 2003 Oct-Dec;28(4):273-8. doi: 10.1007/BF03220179.
Thiourea derivatives have been shown to posses several biological activities. Therefore a series of N-substituted -N'-(3,5-di/1,3,5trimethylpyrazole-4-yl)thioureas were synthesized and the antitubercular and anticonvulsant activities were studied. Among the new compounds, N-phenyl-N'-(3,5-dimethylpyrazole4-yl)thiourea (S) was demonstrated to have remarkable anticonvulsant activity. In this study, S was selected as a model compound and the in vivo metabolic pathway in rats was investigated. The substrate was given intraperitoneally (50 mg/kg) and blood samples were collected at 0, 1, 2, 4, 8, 12, 24 and 48 h. The substrate and its potential metabolites were separated using HPLC on reverse phase system. The substrate was detected at all times with small quantity of metabolites.
硫脲衍生物已被证明具有多种生物活性。因此,合成了一系列N-取代的-N'-(3,5-二/1,3,5-三甲基吡唑-4-基)硫脲,并研究了其抗结核和抗惊厥活性。在新化合物中,N-苯基-N'-(3,5-二甲基吡唑-4-基)硫脲(S)被证明具有显著的抗惊厥活性。在本研究中,选择S作为模型化合物,研究其在大鼠体内的代谢途径。将底物腹腔注射(50 mg/kg),并在0、1、2、4、8、12、24和48小时采集血样。使用反相系统的高效液相色谱法分离底物及其潜在代谢物。在所有时间都检测到底物以及少量代谢物。