Synthesis of new hexahydro- and octahydropyrido[1,2-c]pyrimidine derivatives with an arylpiperazine moiety as ligands for 5-HT(1A) and 5-HT(2A) receptors, Part 2.

The synthesis of new of 4-aryl-hexahydro- (11-16) and (R,R)(S,S)4-aryl-octahydropyrido[1,2-c]pyrimidine (23-27) derivatives bearing a aryl- or heteroarylpiperazinyl moiety in position 2 is described. The derivatives of 4-aryl-hexahydro- (1-5) and (R,R)(S,S)4-aryl-octahydropyrido[1,2-c]pyrimidin-1,3-dion (17-19) served as starting compounds for further synteses. The N-alkylation of the imide moiety in compounds 1-5 and 17-19 by 1,4-dibromobutane gave the respective monbromobutyl derivatives 6-10 and 20-22. The final derivatives 11-16 and 23-27 have been produced by condensation of the obtained bromoderivatives with selected 1-aryl and 1-heteroarylpiperazines. Compounds 11-16 and 23-27 were tested for their affinity towards 5-HT(1A), 5-HT(2A) and alpha1 receptors, using a radioligand binding assay.

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.

Synthesis of N-(4-aryl-1-piperazinylbutyl)-substituted 7,8-benzo-1,3-diazaspiro[4,5]decane-2,4-dione derivatives with potential anxiolytic activity.

Continuing our studies connected with the design of new anxiolytics we have now synthesized a series of new compounds, derivatives of 7,8-benzo-1,3-diazaspiro[4,5]decane-2,4-dione bearing a 4-aryl-1-piperazinylbutyl group attached to the imide nitrogen. One single compound was submitted to the 5-HT1A receptor binding assay and found to display the expected--though rather weak--receptorial affinity.

[Studies of acidic degradation of heparin. A UV-VIS spectroscopy study]. / Badanie produktów kwasowej degradacji heparyny. I. Analiza widmowa.

The preliminary studies on acidic degradation of heparin were performed. The UV-VIS and 1H-NMR techniques were used. The analogical features of degradation products of heparin, glucuronic acid and furfural were found (7 characteristic groups).