[Synthesis and pharmacological properties of fluorostyryl derivatives of 3H-pyrido[2,3]pyrimidine-4-one]. / Synteza i badania farmakologiczne pochodnych fluorostyrylowych 3H-pirydo[2,3-d]pirymidyn-4-onu.

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

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.

Comparison of the electrocortical changes induced by (+)-amphetamine and chlorpromazine when perfused directly into the dorsal raphé nucleus of the cat.

1 (+)-Amphetamine mimicked the intermittent and sustained electrocortical desynchronization produced by (-)-noradrenaline (NA) when perfused directly into the dorsal raphé nucleus of cat encéphale isolé preparations. 2 The effects of amphetamine or NA were abolished or significantly attenuated by prior application of (-)-propranolol. 3 The effect of amphetamine, but not that of NA, was blocked by prior applications of guanethidine or chlorpromazine (CPZ). 4 Desmethylimipramine (DMI) produced dose-related changes in electrocortical activity which were similar to those induced by NA when applied to the same sites within the dorsal raphé nucleus. 5 DMI potentiated the effects of both amphetamine and NA, but guanethidine only abolished the DMI-induced potentiation of the amphetamine response. 6 (-)-Propranolol, guanethidine and CPA produced a short period of electrocortical desynchronization at the beginning of the perfusion period before antagonism of the amphetamine response was apparent. 7 The results suggest that CPZ and amphetamine have an action within the dorsal raphé nucleus possibly related to noradrenergic terminals.

The influence of a new benzonaphtyridone derivative (IFC-45) with antidepressant activity on the central nervous system. Part I. The influence on behaviour and bioelectrical activity of brain.

IFC-45 (10-(3-dimethylaminopropyl)-7-chlorobenzo-[b]-[1,8] naphtyridone-5 monohydrochloride) in small doses, similarly as imipramine and amitryptyline, did not influence animal behaviour. In higher doses it stimulated excitability of animals while imipramine and amitryptyline appeared to have inhibiting action. After IFC-45, desynchronization in EEG was obtained whereas both imipramine and amitryptiline induced synchronization of EEG.

The influence of a new benzonaphtyridone derivative (IFC-45) with antidepressant activity on the central nervous system. Part II. The influence on the amphetamine and reserpine effects and other pharmacological studies.

The Influence of a New Benzonaphtyridone Derivative (IFC-45) with Antidepressant Activity on the Central Nervous System. Part II: The Influence on the Amphetamine and Reserpine Effects and Other Pharmacological Studies. Pol. J. Pharmacol, Pharm. 1975, 27, 479--491. IFC-45 (chem. formula see p. I, page 471) potentiated amphetamine action in a similar manner as standard drugs, had significant but slightly less than the compared standards anti-reserpine activity. IFC-45 did not act anticonvulsivantly, did not affect physostigmine toxicity or evipan anaesthesia.