[Disorders of the bone density in the chest x-ray examination in the course of myelosclerosis]. / Zaburzenia utkania kostnego w obrazie radiologicznym klatki piersiowej w przebiegu zwlóknienia szpiku.

The authors report a rare case of myelosclerosis diagnosed during hospital stay in internal Department on account of hepatosplenomegaly and anaemia. The case of patient described by authors was diagnosed on the ground of examination and executed additional investigations: morphology, peripheral blood picture, chest radiography, scintiscan of skeleton.

[Foreign body in the right frontal lobe of the brain as a result of right eyeball and right eye-socket trauma--case report]. / Cialo obce w prawym placie czolowym mózgu w nastepstwie urazu prawej galki ocznej i oczodolu prawego--opis przypadku.

We report a case of a 44 year old man, who was admitted to our hospital because of right eyeball and right eye-socket due to a piece of diamond circular saw. Right eyeball was sutured. CT--examination showed a metallic foreign body in the right frontal lobe of brain. Metallic foreign body, which damaged the right eyeball, caused upper restriction of right eye-socket ceiling and stuck in a frontal lobe of the brain was removed.

[Gas gangrene or inflammation of the neck--diagnostic difficulties]. / Zgorzel gazowa czy ropowica szyi--trudnosci diagnostyczne.

The authors describe a patient with an extensive inflammation of the neck soft tissues as a complication of the peritonsillar abscess. Follow-up computed tomography revealed gasi-form follicles in the inflammed neck soft tissues, suggesting gas gangrene. We report disseminate ways of the inflammation process on the financial tonsil, reasons of the gangrene also the infections of soft tissues caused by anaerobic bacteries--Clostridium. CT--examination in inflammatory tumors of the neck is valuable, permits to exclude expansion process, but it cannot give unequivocal answer to differentiate gas gangrene and phlegmon.

[Thoracic aortic dissecting aneurysm with bleeding into the pleural cavity]. / Tetniak rozwarstwiajacy aorty piersiowej z krwawieniem do jamy oplucnej.

A rare case of dissecting aneurysm of the aortic arch with left haemothorax was presented. The authors describe modern methods of visualising diagnostics used in case of suspected dissecting aortic aneurysm.

Structure-activity relationship in a series of new 1-(2-pyrimidinyl)piperazine derivatives with hypnotic activity.

Preparation, biological properties and QSAR of new derivatives of 1-[4-(2-pyrimidinyl)-1-piperazinyl]-1, 3-butandione (11-13, and 15-18) and 3-[4-(2-pirimidinyl)-1-piperazinyl]-3-oxopropanoate (20-22) exhibiting hypnotic activity in mice are reported. The best therapeutic indices (TI = LD50/ED50) 4.7 and 9.4 for po and ip administration, respectively, were found for 1-[4-(2-pyrimidinyl)-1-piperazinyl]-2-n-pentyl-1,3-butandione (15). QSAR studies showed that the biological activity grows initially with an increase in lipophilicity to drop dramatically for log P > 2.5.

Some analogues of 1,4-disubstituted piperazines as hypnotic and sedative agents.

Preparation, analytical data, and biological properties such as acute toxicity, influence on spontaneous and amphetamine induced locomotor activity, hypnotic activity, influence on hexobarbital narcosis and anticonvulsant activity of new analogues of pyrimidyl piperazines--ethyl 3-[4-(2-pyrimidyl)-1-piperazinyl]-3-oxopropanoate (4), 1-[4-(2-pyrimidyl)-1-piperazinyl]-1,3-butandione (5), ethyl 3-[4-(2-pyrimidyl)-1-piperazinyl]butanoate (6) and 1-[4-(2-pyrimidyl)-1-piperazinyl]-2-acetyl-1-hexanone (7)--are reported.

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.

Investigations on some pharmacological properties of TPP.

The experiments were performed on mice, rats and rabbits. The influence on circulatory, central nervous, and gastrointestinal system in vivo and in vitro, as well as on renal secretory activity was examined. TPP was administered p.o., i.v. and s.c. at the doses 100.0-400.0 mg/kg. Either in a single dose or multiple doses TPP did not evoke any significant effects (as compared with NaCl solution) on blood pressure, heart and respiratory rate, general behaviour, locomotor activity, body temperature, locomotor coordination, ECoG, smooth muscles of intestine in vivo and in vitro, gastric secretion and on the volume and quality of excreted urine. The augmentation of sodium and potassium ion excretion with urine and slight influence on locomotor coordination both after TPP and 6% NaCl seems to be connected with a high content of salt in TPP.

Synthesis and pharmacological investigations of 3-(aminoalkylene)-1-aryl-2-thioxo-4,5-imidazolidinedione and 2,4,5-imidazolidinetrione derivatives.

New derivatives of 2-thioxo-4,5-imidazolidinedione (3-6, 10, 11) and 2,4,5-imidazolidinetrione (7, 12) were synthesized by N,N'-acylation of asymmetric thioureas and ureas by oxalyl chloride. The obtained compounds were screened for their central action, mainly anticonvulsant activity.

1,3-disubstituted 2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones and their anticonvulsant activity.

New unsymmetrically 1,3-disubstituted derivatives of 2-thioxo-4,5-imidazolidinedione (3, 5-7, 9-12) and 2,4,5-imidazolidinetrione (2, 8, 13-15) were synthesized by condensation of the respective thioureas and ureas with oxalyl chloride. They were screened for their central, mainly anticonvulsant activity and only compound 8 revealed antianxiety and antiepileptic properties.

Aminoacetyl derivatives of 1,5-benzodiazepin-2-one.

A series of six compounds, 5-chloroacetyl-4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one and 5-dialkilaminoacetyl derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one, have been synthesized. 5-Diizobutylaminoacetyl-4-methyl-1H-tetrahydro-1,5-benzodiazepi n-2-one showed weak analgesic and antiinflammatory activity.

Reaction products of dimethyl sulfoxide with 5,5-disubstituted barbituric acids and their biological properties.

In the reaction of 5,5-disubstituted barbituric acids 1-5 with DMSO mixtures of compounds with one (6, 8, 10, 12) or two methylthiomethyl groups (7, 9, 11, 13) at one or both nitrogen atom are formed. Some of obtained compounds were screened for their central action namely anticonvulsant activity.

Synthesis and some biological properties of new derivatives of 1-S-phenylthioglycolonitrile.

A series of new S-phenylthioglycolic acid derivatives was synthetized via common transformations of alkylated S-phenyl-thioglycolonitrile. The compounds were submitted to pharmacological screening. N,N-Diethylaminoethyl ester of 1-S-phenylcyclopentane carboxylic acid was submitted to detailed studies and showed high local anesthetic properties.

Synthesis of new arylanalogs of ketamine.

New, seven-step synthesis of arylanalogs of ketamine, starting from easily available phenylcyclohexane derivatives, is reported. Pharmacological investigations on the compounds obtained are described.