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1.
Bioorg Med Chem Lett ; 23(15): 4419-23, 2013 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-23787101

RESUMO

A series of new xanthone derivatives with piperazine moiety [1-7] was synthesized and evaluated for their pharmacological properties. They were subject to binding assays for α1 and ß1 adrenergic as well as 5-HT1A, 5-HT6 and 5-HT7b serotoninergic receptors. Five of the tested compounds were also evaluated for their anticonvulsant properties. The compound 3a 3-methoxy-5-{[4-(2-methoxyphenyl)piperazin-1-yl]methyl}-9H-xanthen-9-one hydrochloride exhibited significantly higher affinity for serotoninergic 5-HT1A receptors (Ki=24 nM) than other substances. In terms of anticonvulsant activity, 6-methoxy-2-{[4-(benzyl)piperazin-1-yl]methyl}-9H-xanthen-9-one (5) proved best properties. Its ED50 determined in maximal electroshock (MES) seizure assay was 105 mg/kg b.w. (rats, p.o.). Combining of xanthone with piperazine moiety resulted in obtaining of compounds with increased bioavailability after oral administration.


Assuntos
Anticonvulsivantes/síntese química , Piperazinas/química , Xantonas/química , Administração Oral , Animais , Anticonvulsivantes/farmacocinética , Anticonvulsivantes/uso terapêutico , Avaliação Pré-Clínica de Medicamentos , Eletrochoque , Meia-Vida , Cinética , Piperazina , Ligação Proteica , Ratos , Receptor 5-HT1A de Serotonina/química , Receptor 5-HT1A de Serotonina/metabolismo , Receptores de Serotonina/química , Receptores de Serotonina/metabolismo , Convulsões/tratamento farmacológico , Xantonas/farmacocinética , Xantonas/uso terapêutico
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