958852-30-7Relevant academic research and scientific papers
Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: Perhydropyrrole[1,2-a]pyrazines
Dawidowski, MacIej,Herold, Franciszek,Chodkowski, Andrzej,Kleps, Jerzy,Szulczyk, Pawel,Wilczek, Marcin
, p. 4859 - 4869 (2011/11/30)
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.
The synthesis of new diastereomers of (4S,8aS)- and (4R,8aS)-4-phenyl-perhydropyrrole[1,2-a]pyrazine-1,3-dione
Herold, Franciszek,Dawidowski, Maciej,Wolska, Irena,Chodkowski, Andrzej,Kleps, Jerzy,Turlo, Jadwiga,Zimniak, Andrzej
, p. 2091 - 2098 (2008/02/11)
The synthesis of new (4S,8aS)- and (4R,8aS)-4-phenyl-perhydropyrrole[1,2-a]pyrazine-1,3-diones in the cyclocondensation reaction of the respective derivatives of l-prolineamide is described. The effect of the amount of NaOEt, temperature, and reaction time on the proportions of diastereomers formed in the cyclocondensation reaction was examined. The structures of the diastereomers were confirmed by GC/MS, HRMS, HPLC, XRD, and 1H and 13C NMR investigations.
