[Synthesis and pharmacological properties of fluorostyryl derivatives of 3H-pyrido[2,3]pyrimidine-4-one].

The synthesis of fluorostyryl derivatives of 3H-pyrido[2,3]pyrimidine-4-one was described.

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.

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.

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.