Synthesis of N,N'-bis-substituted diimides related to tricyclo [6.2.2.0(1,6)] dodecane with an expected activity on the central nervous system.

Continuing our studies connected with the design of antipsychotic and anxiolytic agents with a reduced propensity toward extrapyramidal side-effects, the synthesis of new compounds related to 3,7-dimethyltricyclo [6.2.2.0(1,6)] dodecen-6-yl-9,10,11,12-tetracarboxydiimide was performed. The first result of the pharmacological screening test of two of synthesized compounds displayed their low affinity for the serotonin receptor site.

Synthesis of new N-[4-(4-aryl- and 4-heteroaryl-1-piperazinyl)butyl]derivatives of 1-methyl-5-oxobicyclo[2.2.1]heptane-2,3-dicarboximide with an expected anxiolytic activity.

Preparation of a number of derivatives of 1-methyl-5-oxobicyclo[2.2.1]heptane-2,3-dicarboximide with a potential anxiolytic activity has been described. New analogs of Tandospirone i.e. derivatives of bicyclo[2.2.1]heptane (10), were aimed at.

Synthesis of N-(4-aryl-1-piperazinylbutyl)-substituted 7,8-benzo-1,3-diazaspiro[4,5]decane-2,4-dione derivatives with potential anxiolytic activity.

Continuing our studies connected with the design of new anxiolytics we have now synthesized a series of new compounds, derivatives of 7,8-benzo-1,3-diazaspiro[4,5]decane-2,4-dione bearing a 4-aryl-1-piperazinylbutyl group attached to the imide nitrogen. One single compound was submitted to the 5-HT1A receptor binding assay and found to display the expected--though rather weak--receptorial affinity.

Synthesis of new N-substituted benzodiazepine derivatives with potential anxiolytic activity.

In continuation of the development of antipsychotic and anxiolytic agents with a reduced propensity toward extrapyramidal side-effects, a series of N-aminoalkyl derivatives of (s)-(+)-2,3-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-(10H, 11aH)-dione was prepared. Evaluation of these compounds in revealed a very low affinity for 5-HT1A receptor.

Synthesis of N,N'-bis-aminoalkyl-substituted derivatives of bicyclo[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide with potential anxiolytic activity.

In continuation of the search for discovering new antipsychotic and anxiolytic agents with a reduced production of extrapyramidala side-effects, a series of N,N'-bis-aminoalkyl derivatives of bicyclo[2.2.2]oct-7-ene tetracarboxydiimide was prepared. Evaluation of these compounds in vitro revealed a very low affinity for 5-HT1A receptor.

Synthesis of novel, aminoalkanolic derivatives of 5,7-dihydroxy-2-phenylbenzopyran-4-on as the potential cytostatic agents.

The 7-(2,3-epoxypropoxy)-2-phenyl-5-hydroxy-4H-benzopyran-4-on and its aminoalkanolic derivatives were prepared as the potential cytostatic (antileukemic) compounds. They were tested in vivo on mice leukemia L1210.

Synthesis and pharmacological profile of bicyclo[2.2.2]octane derivatives: N-(1-aryl-4-piperazinyl-butyl) derivatives of 7-isopropyl-6-methyl- and 1-isopropyl-4-methylbicyclo[2.2.2]oct-5-ene-2,3-dicarboxyimide.

The new class of compounds characterized by anxiolytic or antidepressive properties, including a number of N-(1-aryl-4-piperazinylbutyl) derivatives of the two isomers: 7-isopropyl-6-methyl- and 1-isopropyl-4-methylbicyclo [2.2.2]oct-5-ene-2,3-dicarboxyimide was synthesized. Two compounds were selected for further pharmacological study.

Synthesis and anxiolytic activity of N-substituted cyclic imides N-[4-[(4-aryl)-1-piperazinyl]alkyl]-5,7-dioxabicyclo[2.2.2]octane-2, 3-dicarboximide.

The preparation of N-substituted cyclic imides N-[4-[(4-aryl)-1-piperazinyl]alkyl]-5,7-dioxabicyclo[2.2.2]octane- 2, 3-dicarboximides by condensation of N-(3-chloropropyl)- or N-(4-chlorobutyl)imides with appropriate amine has been described. One of compounds was tested in the Vogel's test and displayed an expected activity on CNS.

Synthesis and pharmacological screening of some N,N'-bis-[4-(4-aryl-1-piperazinyl)butyl]-substituted derivatives of 1,8-dimethylbicyclo-[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide.

The preparation of several derivatives of bicyclo[2.2.2]oct-7-ene- 2,3,5,6-tetracarboxydiimide on two routes has been described. Some of them display an expected anxiolytic activity. The 5-HT1A receptor affinities of tested compounds are comparable with that of buspirone.

Synthesis of some N-substituted derivatives of dibenzo[e.h]bicyclo[2.2.2]octane-2,3-dicarboximide with an expected activity on central nervous system.

The preparation of number derivatives of dibenzo[e.h]bicyclo[2.2.2] octane-2,3-dicarboximide by different routes has been described. One of them displays an expected activity on central nervous system.

Synthesis and central pharmacological screening of new aminoalkoxy derivatives of coumarin and chromene.

Several 8-(2- and 3-aminoalkoxy) derivatives of coumarin and 5-(2- and 3-aminoalkoxy) derivatives of chromene have been synthesized. The strongest, although short-time neurodepressive activity was exhibited by 8-[3-(4-phenyl-1-piperazinyl)propoxy]-7-methoxycoumarin hydrochloride 15.

[Synthesis of aminoalkaloids derived from 8-hydroxy-7-methoxy-2H-1-benzopyran-2-one with expected beta-adrenolytic action]. / Synteza aminoalkanolowych pochodnych 8-hydroksy-7-metoksy-2H-1-benzopiran-2-onu o spodziewanym dzialaniu beta-adrenolitycznym.

Synthesis of 8-hydroxy-7-methoxy-2H-1-benzopyran-2-one and syntheses of several 8-(3-amino-2-hydroxypropoxy)-7-methoxy-2H-1-benzopyran-2-one derivatives with antiarrhythmic activity is described.

[Synthesis of new aminoalkanol derivatives of benzofuran with potential beta-adrenolytic activity]. / Synteza nowych, aminoalkanolowych pochodnych benzofuranu o spodziewanym dzialaniu beta-adrenolitycznym.

Two routes of synthesis of 2-acetyl-7-hydroxy-6-methoxy-3-methylbenzofuran and some of its aminoalkanol ethers are described. Six compounds proved to exert the expected antiarrhythmic and hypotensive effects.

[Synthesis of new derivatives of 5H-furo[3,2-g][1]benzopyran-5-one with potential beta-adrenolytic activity]. / Synteza nowych pochodnych 5h-furo [3-2-g] [1]-benzopiran-5-onu o spodziewanym dzialaniu beta-adrenolitycznym.

With the purpose of obtaining new compounds with antiarrhythmic activity, nine novel aminoalkanol derivatives of 5H-furo[3,2-g] [1]benzopyran-5-one were synthetized. In pharmacological studies, compound IX proved to display strong antiarrhythmic action, which in chloroform-induced arrhythmia was stronger from that of propranolol at three times lower acute toxicity.

[Synthesis of derivative of 2-[4-hydroxy-7-methyl-5-oxo-5H-furo-[3,2g] [1]benzopyran-9-yloxy] acetic and propionic acids with potential effect on the circulatory system]. / Synteza pochodnych kwasów 2-[4-hydroksy-7-metylo-5-okso-5h-furo [3,2-g] [1] benzopiran-9-yloksy] octowego i propionowego o spodziewanym dzialaniu na uklad krazenia.

With the purpose of obtaining new compounds with antiarrhythmic activity, 14 novel derivatives of 5H-furo[3,2-g] [1]benzopyran-5-one were synthetized. Some of them proved to display strong antiarrhythmic action.