☆ 4.7 Article

Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: Perhydropyrrole[1,2-a]pyrazines

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2011)

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

卷 46, 期 10, 页码 4859-4869

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

DOI: 10.1016/j.ejmech.2011.07.027

关键词

2,6-Diketopiperazine; 2,6-Piperazinedione; Pyrrole[1,2-a]pyrazine; Anticonvulsant activity; Chirality; Conformational analysis

类别

Chemistry, Medicinal

资金

Committee for Scientific Research, Poland [N N405 623138]

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摘要

A number of novel pyrrole[1,2-a]pyrazine derivatives were synthesized and evaluated in in vivo animal models of epilepsy. Among them, several compounds displayed promising seizure protection in the maximal electroshock seizure (MES), subcutaneous metrazol seizure (scMET), 6 Hz and pilocarpine-induced status prevention (PISP) tests, with ED50 values comparable to the reference anticonvulsant drugs (AEDs). A critical influence of the stereochemistry and conformational preferences of the pyrrole[1,2-a]pyrazine core on in vivo pharmacological activity was observed. The mechanism of the anticonvulsant action of the agents synthesized is most probably not via inhibition of the voltage-dependent sodium (Na+) currents. (C) 2011 Elsevier Masson SAS. All rights reserved.

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