Jerzy Modzelewski

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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(More)
Two series of N10 substituted derivatives of 1,3-dimethyl-2,4,9-trioxo-1,3,6,7,8,10-hexahydro-1,3-diazepino+ ++-[2,1-f]- purine and 1,3-dimethyl-2,4-dioxo-1,3,6,7,8,9-hexahydro-10H-1,3-dizepino- [2,1-f]-purine were synthesized and tested for CNS activity. The most active in central nervous system tests were compounds [II] and [XIV].
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.
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.(More)
Following a research program on piperazinoalkyl-substituted tricyclic purines, a number of N-9-aryl(alkyl)-piperazinopropyl substituted tetrahydropyrimido-[2,1-f]-purines were synthesized and tested pharmacologically with respect to their influence on the central nervous system. Two of the new compounds induced hypothermia and decreased the spontaneous(More)
The three different kinds of imidazo[2,1-f]theophylline derivatives were synthesized and tested for their CNS activity. A series of alkoxy-alkylamides and amino-alkylamides with basic function, derived from 8-benzyl-6,7-dihydroimidazo[2,1-f]theophylline-7-carboxylic acid showed stimulating influence on CNS as they increased the locomotor activity (compound(More)
Synthesis and the results of preliminary pharmacological evaluation of four new 9-substituted pyrimidino[2,1-f]purines, containing pyrimidinyl-piperazine substituent are described. Some of these substances induced hypothermia, antagonism of amphetamine action and neurotoxic effects. All compounds had weaker activity on the central nervous system than(More)