Evaluation of anticonvulsant and analgesic effects of benzyl- and benzhydryl ureides

Librowski, Tadeusz; Kubacka, Monika; Meusel, Manuela; Scolari, Silvia; Müller, Christian; Gütschow, Michael

doi:10.1016/j.ejphar.2006.12.002

Cited by 16 publications

(16 citation statements)

References 48 publications

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“…1 These agents mainly affect transport of ions across the cell membrane and/or modulate inhibitory or excitatory neurotransmission. 2 A wide array of adverse effects associated with these agents are a major limitation for their long term use. 3 Therefore, the development of a novel antiepileptic agent with better efficacy and minimal adverse effects would be an interesting prospect in the field of medical research.…”

Section: Introductionmentioning

confidence: 99%

Trimetazidine exerts protection against increasing current electroshock seizure test in mice

Jain

Bharal

Mediratta

et al. 2010

Seizure

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Trimetazidine, a novel anti-ischemic agent, is used in the therapy of angina, vertigo and chorioretinal diseases. It has also been examined for its effect on nociception, inflammation and neuroprotection in various animal models. The present study was designed to investigate the effect of trimetazidine on electrically induced seizures in mice. Trimetazidine was administered orally in doses of 5, 10 and 20mg/kg (single dose) to observe its effect on the increasing current electroshock seizure (ICES) test in mice. Trimetazidine in 10 and 20mg/kg doses significantly raised the seizure-threshold current in the ICES test. Further, co-administration of per se ineffective dose of trimetazidine (5mg/kg, p.o.) with sub-anticonvulsant dose of nimodipine (10mg/kg, p.o.) and phenytoin (12.5mg/kg, p.o.) offered significant protection in the ICES test. These results indicate that trimetazidine possesses significant anticonvulsant activity against electro-convulsions in the mice.

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Section: Introductionmentioning

confidence: 99%

Trimetazidine exerts protection against increasing current electroshock seizure test in mice

Jain

Bharal

Mediratta

et al. 2010

Seizure

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“…1) to explain some of the physicochemical processes that occur with the participation of this compound. The studies carried out in the field of urea chemistry made it possible to create a variety of biologically active and other compounds of acyclic and heterocyclic structures containing the urea NH-CO-NH fragment [6][7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

1D and 2D NMR spectroscopy for identification of carbamide-containing biologically active compounds

Бакибаев¹,

Panshina²,

Ponomarenko³

et al. 2021

Bull. of the Kar. Univ. "Chem". Ser.

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Urea (carbamide) is the main end product of amino acids' metabolism in mammals. Extensive research in the field of urea chemistryhas contributed to the creation of many biologically active and other compounds based on the carbamide fragment NH–CO–NH. The substituting groups of urea directly affect its properties and characteristics which are reflected in the NMR spectral data and this circumstance can be the basis for the identification of urea derivatives. In this work, chemical shifts in the NMR spectra of urea and its acyclic structure, barbituric series, imidazolidinone series and bicyclic structure derivativeswere studied and identi-fied. A system analysis was carried out to determine the effect of the type of substituents on the positions of signals of the NH-CO-NH fragment in the NMR spectra. The possibility of 2D NMR spectroscopy using to simplify the identification procedurefor complex mixtureswas shown in the paper. The combined use of 1D and 2D NMR spectroscopy is convenient and informative to establishthe structure of biologically active compounds. These methods make it possible to determine the presence and type of impurities, as well as to establish thedestruction processes leading to the corresponding impurities.

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“…Anticonvulsive activity of hydantoins is mediated by their interaction and inhibition of the voltage‐gated sodium channels in the brain. The investigation has shown that the structural fragments involved in anticonvulsant activity are heterocyclic ring, at least 1 carbonyl group, and lipophilic phenyl or alkyl/cycloalkyl substituent attached to the heterocyclic system …”

Section: Introductionmentioning

confidence: 99%

Chromatographic and in silico assessment of logP measures for new spirohydantoin derivatives with anticancer activity

Sekulić

Smoliński

Mandić

et al. 2017

Journal of Chemometrics

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Lipophilicity has, for a long time, been recognized as a meaningful parameter in structure-activity relationships. It is also the single most informative physicochemical property that reveals a wealth of information on intermolecular forces, intramolecular interactions, and molecular structure in the broadest sense. In this paper, a total of 14 chromatographic measures of lipophilicity (thin-layer chromatography and high-performance liquid chromatography) and 11 computationally estimated logP-s for 21 newly synthesized 3-(4substituted benzyl)-cycloalkylspiro-5-hidantoin derivatives have been investigated. Similarities among the investigated compounds as well as lipophilicity measures were examined by the multivariate exploratory analysis, principal component analysis, hierarchical cluster analysis, and sum of ranking differences. These chemometric approaches reveal the arrangement of investigated compounds into clusters according to lipophilicity. Chemometric consideration of lipophilicity renders principal component scores as entirely unsuitable lipophilicity measures. Furthermore, the logP values estimated from calibration graph by using a set of standard reference compounds were equivalent to the corresponding chromatographic descriptors of hydantoins extrapolated from linear relationship between retention parameters and mobile phase composition. Comparison of the 2 chromatographic techniques places high-performance liquid chromatography lipophilicity indices slightly ahead of thin-layer chromatography.

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Evaluation of anticonvulsant and analgesic effects of benzyl- and benzhydryl ureides

Cited by 16 publications

References 48 publications

Trimetazidine exerts protection against increasing current electroshock seizure test in mice

Trimetazidine exerts protection against increasing current electroshock seizure test in mice

1D and 2D NMR spectroscopy for identification of carbamide-containing biologically active compounds

Chromatographic and in silico assessment of logP measures for new spirohydantoin derivatives with anticancer activity

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