Synthesis and hypotensive activity of some heterocyclic analogues of GYKI-12 743.

[1,4]Benzodioxanylmethyl-, [1,4]benzodioxanylmethylaminopropyl- and phenoxyethylaminoethyl-substituted lactams were synthesised and their hypotensive activity was investigated. Some of these compounds show moderate to high hypotensive effect, but they had more toxic and/or side effects than GYKI-12 743.

Synthesis of pyridylthiazoles as antisecretory agents.

4-(3-Pyridyl)thiazole and 2-methylimidazo[1,2-a]pyridine derivatives with anticholinergic antisecretory activity were synthesized. Most of the compounds (3-16) were formed from carbohydrazide 2 and carbonitrile 9. Some thiazole derivatives, most of them containing nitrogen attached to the thiazole C-2 (19-20), were prepared from 17 and 18 by known method.

The CNS effects of 5-aminobenzoic acids inhibiting the biosynthesis of prostaglandins.

It was found that the 2,5-diaminobenzoic acid derivatives 1 activating the biosynthesis of prostaglandins have CNS side effects. The replacement of the 2-NH group in 1 by O or S resulted an inhibition of prostaglandin biosynthesis and increased CNS activity.

Synthesis of thiazole derivatives with positive inotropic effect.

Thiazole derivatives with potential positive inotropic effect were synthesized. The highest activity (medium positive inotropic effect) was exhibited by ethyl 2-(2-hydroxyethylamino)-4-phenylthiazole-5-carboxylate (3b) of which several derivatives have been prepared. Among these derivatives only those which could presumably easily removed in the living organism to give 3b exhibited a medium positive inotropic effect (6, 8b).

Studies in the field of pyridazine compounds. Part 21. Structural studies on 6-H-pyrimido[1,2-b]-1,2,4-triazolopyridazines.

The structure of 7,8-dihydro-6H-pyrimido [1,2-b]-1,2,4-triazolo [3,4-f] pyridazine (2a) was confirmed by 1H and 13C NMR spectroscopy and by preparation of the isomeric [5,1-f] pyridazine 3. Some derivatives of 6H-pyrimido [1,2-b]-1,2,4,-triazolo [3,4-f]pyridazine were prepared. Compounds 2a, 2b and 9a showed a positive inotropic effect.