Literature DB >> 14743968

In vivo metabolism of N-phenyl-N'-(3,5-dimethylpyrazole-4-yl) thiourea in rats.

Bedia Koçyiğit Kaymakcioğlu1, Sevim Rollas, Feyza Kartal-Aricioğlu.   

Abstract

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.

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Year:  2003        PMID: 14743968     DOI: 10.1007/BF03220179

Source DB:  PubMed          Journal:  Eur J Drug Metab Pharmacokinet        ISSN: 0378-7966            Impact factor:   2.441


  15 in total

1.  Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.

Authors:  Y Dong; T K Venkatachalam; R K Narla; V N Trieu; E A Sudbeck; F M Uckun
Journal:  Bioorg Med Chem Lett       Date:  2000-01-03       Impact factor: 2.823

2.  Synthesis and antihypertensive activity of N-(alkyl/alkenyl/aryl)-N-heterocyclic ureas and thioureas.

Authors:  O Vajragupta; A Pathomsakul; C Matayatsuk; L Ruangreangyingyod; Y Wongkrajang; W O Foye
Journal:  J Pharm Sci       Date:  1996-03       Impact factor: 3.534

3.  The in vivo metabolism of 5-(4-nitrophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione in rats.

Authors:  E E Oruç; S Rollas; L Kabasakal; M K Uysal
Journal:  Drug Metabol Drug Interact       Date:  1999

4.  N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.

Authors:  F M Uckun; S Pendergrass; D Maher; D Zhu; L Tuel-Ahlgren; C Mao; T K Venkatachalam
Journal:  Bioorg Med Chem Lett       Date:  1999-12-20       Impact factor: 2.823

5.  [Derivatives of thiourea and their antitubercular activity].

Authors:  F M Riccieri; G A Porcelli; M Castellani Pastoris
Journal:  Farmaco Sci       Date:  1967-02

6.  Synthesis, characterization and evaluation of antituberculosis activity of some hydrazones.

Authors:  Kaymakçioğlu B Koçyiğit; S Rollas
Journal:  Farmaco       Date:  2002-07

7.  Physiologic disposition and metabolism of an anti-ulcer agent, N-(2-diisopropylaminoethyl)-N-(4,6-dimethyl-2-pyridyl)-N',N'-dimethylurea, in rats, dogs, and monkeys.

Authors:  H B Hucker; S C Stauffer; S D White; B H Arison; A G Zacchei
Journal:  Drug Metab Dispos       Date:  1982 Jan-Feb       Impact factor: 3.922

8.  Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.

Authors:  F W Bell; A S Cantrell; M Högberg; S R Jaskunas; N G Johansson; C L Jordan; M D Kinnick; P Lind; J M Morin; R Noréen
Journal:  J Med Chem       Date:  1995-12-08       Impact factor: 7.446

9.  Synthesis and characterization of certain thiourea derivatives starting from 1,2,4-triazoline-3-thiones as potential antibacterial and antifungal agents.

Authors:  I Küçükgüzel; S Rollas; A Cevikbaş
Journal:  Drug Metabol Drug Interact       Date:  1995

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

Authors:  N N Gülerman; E E Oruç; F Kartal; S Rollas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2000 Apr-Jun       Impact factor: 2.569

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  5 in total

1.  In vivo metabolism of 2-[1'-phenyl-3'-(3-chlorophenyl)-2'-propenylyden]hydrazino-3-methyl-4(3H)-quinazolinone in rats.

Authors:  Bedia Koçyiğit Kaymakçioğlu; Yasemin Aktan; Sibel Süzen; Nesrin Gökhan; Semra Koyunoğlu; Kevser Erol; Akgül Yeşilada; Sevim Rollas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2005 Oct-Dec       Impact factor: 2.441

2.  High pressure liquid chromatographic analysis of in vivo metabolites of N-(substituted phenyl)-N'-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats.

Authors:  Bedia Kocyigit-Kaymakcioglu; Ufuk Yilmaz; Feyza Aricioglu
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2007 Oct-Dec       Impact factor: 2.441

3.  The in vivo metabolism of 3-oxo-5-benzylidene-6-methyl-(4H)-2-(benzoylmethyl)pyridazine in rats.

Authors:  E Elçin Oruç; Oya Unsal; Ayla Balkan; Fügen Ozkanli; M Zafer Gören; Berna Terzioğlu; Sevim Rollas
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2006 Jan-Mar       Impact factor: 2.441

4.  A comparative study of the metal binding behavior of alanine based bis-thiourea isomers.

Authors:  Imran Fakhar; Bohari M Yamin; Siti Aishah Hasbullah
Journal:  Chem Cent J       Date:  2017-08-04       Impact factor: 4.215

5.  Design, Synthesis and Biological Evaluation of Benzo[D]Thiazole with Dimethylpyrazol Derivatives.

Authors:  Dachuan Liu; Xiu Cheng; Ying Wang
Journal:  Asian Pac J Cancer Prev       Date:  2019-11-01
  5 in total

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