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The present paper reports on the synthesis and preliminary pharmacological properties of N-[beta-hydroxy-gamma-(N-phenylpiperazinepropyl)]-2- pyrrolidinone (MG-1). MG-1 was obtained by aminolysis of 1-(beta, gamma-epoxypropyl)-2-pyrrolidinone and N-phenylpiperazine. Its structure was established by elemental and spectral analyses (IR, UV, MS, 1H, 13C, 2D H-H and 2D C-H NMR). The antiarrhythmic activity of MG-1 was investigated on mice, rats and guinea pigs, using several models of arrhythmia. MG-1 attenuated or prevented the adrenaline- and barium chloride-induced arrhythmia. MG-1 demonstrated potent local anesthetic properties and depressed the depolarization phase of the action potential of cardiac cells. These results indicate that MG-1 possesses antiarrhythmic activity.

Two series of N9-alkylaminomethyl-, alkylpiperazino-, alkylpiperidino-substituted 1,3-dimethyl-(hexahydropyrimidino)- and (tetrahydropyrimidono)-[2,1-f]-purines were prepared and their physicochemical and pharmacological properties were described. The most active in central nervous system tests were the compounds with phenylpiperazinealkyl substituent i.e. 1,3-dimethyl-2,4-dioxo-9-[N1N4-(phenyl)-piperazinopropyl]-1, 3,6,7,8,9- hexahydropyrimidino-[2,1-f] purine 6a and its butyl and isobutyl homologs 9 and 12. The compounds depressed statistically significantly spontaneous locomotor and amphetamine activity and showed sedative, analgetic and hypothermizing properties.

Synthesis, chemical properties and results of preliminary pharmacological evaluation of several new 9-substituted pyrimidino-[2,1-f]-purines are described. The most interesting was 1,3-dimethyl-2,4,8-trioxo-9-[gamma-N1-(N4-C6H5)-piperazynopropy l]-1,3,6,7-tetrahydro-9H-pyrimidino-[2,1-f]-purine (compound 4a), which exerted strong sedative, hypothermizing and cataleptogenic action and possessed some anti-amphetamine and anti-apomorphine properties.

Synthesis and properties of new N-substituted amides of alpha-(1,1-ethylenedioxy)-ethyl-gamma-hydroxybutyric acid are described. The compounds were obtained by aminolysis of 3-(1,1-ethylenedioxy)-ethyltetra-hydrofuran-2-on with primary alkylarylamines. Preliminary pharmacological assessment revealed that the compounds exert weaker influence on the central nervous system than the reference gamma-hydroxybutyric acid. Three of the novel compounds offered some protection against pentetrazole-induced tonic seizures in mice.

In a search for new compounds with cardiovascular activity several derivatives of 8-benzylaminotheophylline with hydroxyalkyl and hydroxyalkylamino substituents at 7-position have been obtained. Some of these compounds were screened for their hypotensive activity.

N-aminoalkyl derivatives of 2-pyrrolidinone (1-5) and methylene-bis-amino derivatives (7-9) as intermediary products formed during aminoalkylation were described. Compounds 2 and 3, in doses over 30 and 20 mg/kg resp., displayed analgesic properties; compound 3 exerted also a weak anti-inflammatory action (37 mg/kg po) in the carrageenin test.

The paper describes the mode of obtaining and physico-chemical properties of new 1-(beta-hydroxy-gamma-aminopropyl)-2-pyrrolidinone derivatives and their antiarrhythmic effect and the action on the circulatory system.

In order to examine the circulatory and bronchospasmolytic activity, new 7-beta-hydroxy-gamma-N4-alkylpiperazinopropyl-8- benzylaminotheophyllines (1, 2, 3) were synthesized and converted to the water soluble dihydrochlorides (1a, 2a, 3a). They showed hypotensive and bronchodilatory effect.

The synthetic routes leading to 7-beta-hydroxyethyl- (I) and 7-beta-hydroxypropyl-8-benzylaminotheophylline (II) were described. Particularly the opening of oxazolidine ring in easy available oxazolidine-(2,3-f)-theophyllines with benzylamine was investigated. The structure of I, II and acetyl derivatives Ia, Ib, IIa and IIb was also confirmed by UV spectra.

Methods of synthesis, chemical properties and results of preliminary pharmacological screening for 8-amino substituted derivatives of caffeine (1-3) and 7,8-disubstituted derivatives of 8-aminotheophylline (8-12) have been described. The compounds show weak sedative and antidepressive activity and some of them (2, 10, 12) also small antinociceptive effect.

A series of 2-piperidino-(1a-k) and 2-homopiperidino-(2a-k)-tetrahydropyrimidine-4,6-diones was synthesized. The structure of the compounds was confirmed by elemental analysis and UV spectra. Compounds 1a, 1j, 2a and 2k showed the antidepressant activity.

We described synthesis of 1-aryl-3 and 5-substituted 2-pyrrolidinones (2a--5a and 3b--4b). Pharmacological studies revealed that compounds 3b, 4a and 4b have analgetic and antiinflammatory properties. None of the compounds posesses neuroleptic or anticonvulsant properties.