Synthesis, pharmacological activity and nitric oxide generation by nitrate derivatives of theophylline.

Nitrates of theophylline derivatives - potential nitric oxide (NO) donors - were synthesized by esterification of 7-hydroxyalkyl theophylline derivatives with fuming nitric acid. The nitrates obtained were tested in-vitro in reactions with sulfydryl compounds at appropriately adjusted pH and temperature. Under the applied conditions, the synthesized compounds underwent decomposition to release NO, quantified using a polarographic method using a selective isolated (ISO-NO) sensor.

A new nitrate derivative of piperazine: its influence on platelet activity.

Nitric oxide (NO) is a potent vasodilator and inhibitor of platelet activation. Its donors, organic nitrates, are still a main group of drugs administered in ischaemic heart disease. The aim of this study was to investigate the effect of a new NO-donor analogue, 1-(3-piperidinepropionyl)-4-(2-nitrooxy-3-piperidinepropyl) piperazine trihydrochloride (NO-P), on platelet activity.

Study on organic nitrates, part VIII. Pharmacological activity and nitric oxide generation capacity of nitrate derivatives of piperazine.

Organic nitrates, derivatives of piperazine, incubated with L-cysteine hydrochloride in phosphate buffer at appropriately high pH and temperature underwent decomposition, releasing nitric oxide (NO). NO generated in this reaction was quantitated by polarographic method using a selective ISO NO sensor. Spontaneously hypertensive rats were used in the tests of hypotensive activity of both investigated organic nitrates and their hydroxyl analogues.

A study on organic nitrates, Part VI. Synthesis and pharmacological activity of 1-isopropylamino-3-(1-naphthyloxy)-2-propyl nitrate.

Basing on the studies on the relationship between the structure and activity, we have synthesized a nitrate analogue of propranolol as potential donor of nitric oxide. The obtained 1-isopropylamino-3-(1-naphthyloxy)-2-propyl nitrate decreases blood pressure more than propranolol and slows the heart rate less than propranolol. It also affects peripheral vascular resistance less than propranolol.

The study on organic nitrates, part V. New derivatives of piperazine potential NO donors.

We have obtained a series of non-symmetrical 1,4-disubstituted derivatives of piperazine, with the structure of organic nitrates, as potential NO donors. These compounds were obtained from respective hydroxyl derivatives of piperazine in an esterification reaction by fuming nitric acid. The obtained nitrates were tested in-vitro by reaction with a sulfhydryl compound.