Synthesis and pharmacological properties of derivatives of isoxazolo[4,3-d]pyrimidine. III.

Synthesis of new isoxazolo[4,5-d]pyrimidine derivatives is reported. Some of isoxazolo[4,5-d]pyrimidine derivatives were tested for anticonvulsant, anxiolytic and antiserotonine activity. Compounds 14 and 16 proved active against hypothermia induced by reserpine and hyperthermia induced by m-CPP.

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.

Repeated diazepam administration influences 5-HT1A receptor binding in the rat brain.

Repeated administration of diazepam for 14 days (5 mg/kg daily) resulted in a significant increase of 5-HT1A receptor density in the midbrain of the rat. Bmax values were increased from 239.6 to 684.9 fmol/mg. The affinity constants (KD) were also increased, from 0.97 to 3.01 nM/l.

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 and pharmacological screening of derivatives of isoxazolo[4, 3-d]pyridimidine.I.

The synthesis of new derivatives of isoxazole and new derivatives of isoxazolo[4,3-d]pyridine is described. The anticonvulsant and anxiolytic activity of some isoxazolo[4,3-d]pyrimidine derivatives was tested in a preliminary screening.

Synthesis and preliminary pharmacological assessment of derivatives of isoxazolo[4,3-d]pyrimidine. II.

Some new derivatives of 5-alkylaminomethyl-3-benzoyl-7-oxo-6,7-dihydroisoxazolo[4,3- d]pyrimidine [II-VI] and 7-amine substituted 3-benzoyl-5-phenylisoxazolo[4,3-d]pyrimidine [VIII-X] were synthesized. Preliminary results of pharmacological screening of compounds synthesized as [II-V,IX,X] have been presented.

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 pharmacological investigation of new N-dimethylpyridyl and N-chloropyridyl substituted arylsuccinimides.

In the reaction of alpha-phenyl-, alpha-p-chlorophenyl-, alpha-m-chlorophenyl-, alpha-p-bromophenyl and alpha-m-bromophenyl succinic acids with various aminopyridines, N-(dimethylpyridine)-alpha- arylsuccinimides and N-(chloropyridine)-alpha-arylsuccinimides were obtained. The above compounds tested for their CNS activity did not show an anticonvulsant activity.