Biomedical subjects
Publications and source records attributed to L Korzycka.
The synthesis and biological activity of a series of 6-oxo-1,2,3,4-tetrahydro-6H-pyrimido[2,1-b]quinazoline is reported. Pharmacological investigations have shown that the compounds exert depressive action on the central nervous system and exhibit neuroleptic activity.
The reaction of N-(1-methylethyl)-3-(1-naphthalenyloxy)-2-nitroxypropylamine (nitrate analogue of propranolol) with hydrochloride of ethyl ester of L-cysteine at pH 7.7, temp. 37 degrees C was studied. The course of the reaction was monitored by HPLC method. It was found that at these conditions the substrates react and the main product of the decomposition of the nitrate of propranolol analogue is propranolol, nitrate and nitrite ions. The reaction has been described qualitatively and quantitatively. The influence of nitrate analogue of propranolol and propranolol alone on arterial blood pressure and heart rate in normotensive and hypertensive rats (SHR) was also studied. It has been found that both compounds exert a similar effect.
By direct acylation of piperazine with halogenocarboxylic acid chlorides in acid medium, the hydrochlorides of 1-haloacylpiperazines were obtained.
New asymmetric piperazines 1-6 were obtained by condensation of 1-acylpiperazines with 1,2-epoxy-3-chloropropane, 1,2-epoxypropane, arylacid chlorides and secondary amines. The compounds displayed a biological activity: they depressed the central nervous system, altered the blood pressure, and one of them increased the coronary flow.
New asymmetric piperazines 9-19 were obtained by condensation of 1-acyl-piperazines with 1,2-epoxy-3-chloropropane, arylacid chlorides, phenols, amines and 1-(alpha-naphthyloxy)-2,3-epoxypropane. Most of the compounds produced a transient hypotension and exerted a spasmolytic action of the isolated intestine. Compounds 10, 11 and 13 displayed a weak antiarrhythmic effect in the adrenaline arrhythmia test in rats. Compounds 14 and 15 increased the coronary flow, but their action was weaker than that of compound 4, described in the first part of the paper.
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The condensation of asymmetrically substituted 1,4-bis(haloacyl) piperazines with secondary amines yielded asymmetric 1,4-bis (aminoacyl) piperazines 3-6, which were further transformed into the respective dimethiodides 3b-6b by treatment with methyl iodide. Those compounds were found to inhibit the neuromuscular transmission by blocking the motor end-plate receptors. Compounds containing piperidine moiety and branched acyl chain 4b displayed enhanced activity.