Synthesis and conformational analysis of 3-substituted derivatives of 1H, 3H-pyrido[2,3-d]pyrimidin-4-one of expected depressive activity on central nervous system. Part II.

Two series of new 1-aryl piperazinylacetyl derivatives of 1H, 3H-pyrido[2,3-d]pyrimidyn-4-one were synthesized. The compounds were prepared by chloroacetylation; when made to react with respective arylpiperazine, then yielded VIa-o. The structures of compounds VIa-o were analyzed by 1H and 13C NMR spectroscopy. For selected compounds, acute toxicity and anticonvulsant activity were determined.

Syntheses of some amide and ester derivatives of 6-methyl-2-pyridinecarboxylic acid of expected activity on circulatory system.

Syntheses of some 6-methyl-2-pyridinecarboxylic acid derivatives in condensation reaction of selected amines and alcohols with acyl chloride and mixed anhydrides were described.

Synthesis of pyridylethenyl derivatives of 3H-pyrido[2,3-d]-pyrimidyn-4-on of expected depressive activity on central nervous system. Part I.

Synthesis of 2-(pyridylethenyl) derivatives of 3H-pyrido[2,3-d]pyrimidin-4-on [Va-k] by condensation of selected 2-methyl-3H-pyrido[2,3-d]pyrimidin-4-ones [IVa-k] with nicotinic aldehyde is described. Compounds [Vh] and [Vi] showed weak analgetic activities.

The synthesis and pharmacological activity of two new derivatives of benzazocine.

Two new derivatives of benzazocine of anticipated analgesic action were synthesized. Pharmacological investigations were carried out to confirm their analgesic activity, affinity to the opiate receptor and potential antagonistic properties.

[Synthesis of certain derivatives of 3-(N'-substituted)acetamide hydantoin and predicted pharmacologic action]. / Syntezy niektórych pochodnych3-(N'-podstawionych)acetamidohydantoinyo spodziewanym dzialaniu farmakologicznym.

Synthesis of 5,5-disubstituted derivatives of 3-N'-(diethyl-, isopropyl- and diphenyl-)-acetamidhydantoin is described.

[Synthesis of derivatives of 2,4-bis(arylmethino)-8-butyl-8- azabicyclo[3.2.1]octan-3-one]. / Syntezy pochodnych 2,4-bis(arylometino)-8-butylo-8-azabicyklo [3.2.1] oktan-3-onu.

In the frame-work of continued search for novel compounds with potential cholagogic or antitumour activity, some derivatives of 2,4-bis-(arylmethino)-8-butyl-8-azabicyclo[3.2.1]octan-3-one were synthesized. 8-Butyl-8-azabicyclo[3.2.1]octan-3-one was condensed with selected tolualdehydes, methoxybenzaldehydes and chlorobenzaldehydes, as well as with piperonal, furfural, dimethylaminobenzaldehyde, 3-pyridine-carboxaldehyde and 4-pyridine-carboxaldehyde. Products of these reactions were isolated in the form of free bases or their hydrochlorides. The obtained compounds were subjected to pharmacological studies. Two as yet investigated compounds failed to induce statistically significant increase in the volume of secreted bile, but one of them was found to display cholinergic activity.

Analgesic activity and opiate receptor affinity of new derivatives of N-butylpiperidine.

The three newly synthesized derivatives of N-butylpiperidine 1-butyl-4-phenyl-4-isonicotinoylaminoethylpiperidine (BG 25), 1-buty-isonicotinoylpiperidine (BG 26) and N-(1-butyl-4-phenyl-4-piperidinoyl) tetrahydropapaverine (BG 9) were evaluated for analgesic activity and opiate receptor affinity. All the three compounds showed analgesic activity both in hot-plate and flinch-squeak-jump test in mice, BG 9 being the most potent. The affinity of the compounds to opiate receptor was moderate (in comparison with pentazocine): the affinity of BG 9 was much greater than that of BG 25 and BG 26. The compounds showed a pronounced inhibitory action in stimulated guinea-pig ileum preparation; this was reversible by naloxone. As evaluated on pA basis, all three investigated compounds showed moderate antagonistic activity. Also in this respect BG 9 was more active than the other two compounds. Cholinolytic and strong spasmolytic properties were observed in isolated rat ileum preparation for BG 9 only.