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Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone

Anticonvulsant evaluation of aminoalkanol derivatives ...

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dc.contributor.author Szkaradek, Natalia [SAP20002583] pl
dc.contributor.author Gunia-Krzyżak, Agnieszka [SAP20003022] pl
dc.contributor.author Waszkielewicz, Anna [SAP20012444] pl
dc.contributor.author Antkiewicz-Michaluk, Lucyna pl
dc.contributor.author Cegła, Marek [SAP20001397] pl
dc.contributor.author Szneler, Edward [SAP11009970] pl
dc.contributor.author Marona, Henryk [SAP20000903] pl
dc.date.accessioned 2015-01-20T13:21:56Z
dc.date.available 2015-01-20T13:21:56Z
dc.date.issued 2013 pl
dc.identifier.issn 0968-0896 pl
dc.identifier.uri http://ruj.uj.edu.pl/xmlui/handle/item/2636
dc.language eng pl
dc.title Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone pl
dc.type JournalArticle pl
dc.description.physical 1190-1198 pl
dc.abstract.en A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested substances showed protection against electrically evoked seizures in the majority of the tested mice at the dose of 100 mg/kg. Additionally, one was effective at the dose of 30 mg/kg. Five substances were active at the dose of 300 mg/kg or at the dose of 100 mg/kg in the minority of the tested mice. The most promising compound revealed ED50 value of 47.57 mg/kg in MES (mice, ip, 1 h after administration) and at the same time its TD50 was evaluated as above 400 mg/kg. Those values gave PI (calculated as TD50/ED50) of more than 8.41. Three other synthesized xanthone derivatives also proved to act as anticonvulsants and showed ED50 values in MES test (mice, ip) ranged 80–110 mg/kg. Results were quite encouraging and suggested that in the group of xanthone derivatives new potential anticonvulsants might be found. pl
dc.subject.en anticonvulsant pl
dc.subject.en MES pl
dc.subject.en neurotoxicity pl
dc.subject.en xanthone pl
dc.subject.en synthesis pl
dc.description.volume 21 pl
dc.description.number 5 pl
dc.description.points 30 pl
dc.identifier.doi 10.1016/j.bmc.2012.12.051 pl
dc.identifier.eissn 1464-3391 pl
dc.title.journal Bioorganic & Medicinal Chemistry pl
dc.language.container eng pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Bioorganicznej pl
dc.affiliation Wydział Chemii : Pracownia Spektroskopii NMR pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Organicznej pl
dc.subtype Article pl
dc.rights.original bez licencji pl
.pointsMNiSW [2013 A]: 30


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