[Benzimidazo-pyrimidino-imidazo-thiadiazines pharmacologically active]. / Benzimidazo-pirimidino-imidazo-tiadiazine farmacologic active.

UNLABELLED: The compounds with thiadiazine structure have numerous biological properties. They are known for antimycotic, antimicrobial, antiviral, vasodilatatory, antiarytmic, bronhodilatatory and antiagregant actions. MATERIAL AND METHOD: In order to study the influence of the different substituents on pharmacological properties of the thiadiazine compounds new benzimidazo-pyrimidino-imidazo-thiadiazine derivatives with potential biological actions have been synthesized. RESULTS: The optimal conditions of reaction have been established and the chemical structure of the synthesized compounds has been confirmed by elemental analysis and IR spectroscopy. CONCLUSIONS: The calculated formula according to the elemental analysis results and the spectral characteristics are in good agreement with the expected structures proposed.

[Synthesis and physico-chemical characterisation of some new derivatives of rutoside and clofibric acid]. / Sinteza si caracterizarea fizico-chimica a unor noi compusi ai rutozidului cu acidul clofibric.

Fibrates are drugs with efficacy in reducing blood cholesterol levels and especially, triglyceride plasma levels. Unfortunately, fibrates have a poor water-solubility and showed some adverse reactions at long treatment. The objective of this study was to obtain some new clofibric acid derivatives with rutin; some of these compounds contain a guanidine moiety, known as effective at cardiovascular level. All the compounds are soluble in water.

[Researches on methyl-xanthine series.XI. Synthesis and physicochemical characterization of some 7-R-1,3-dimethyl-xanthine derivatives]. / Cercetari în seria metil-xantinelor. Sinteza si caracterizarea fizico-chimica a unor 7-R-1,3-dimetil-xantine.

We have synthesized new xanthine compounds, derivatives of theophylline with various radicals in 7 position. The compounds have been characterized by molecular formula, weight, yield and melting point. The synthesized xanthine derivatives have been purified by repeated crystallizations from various organic solvents. Their chemical structure was confirmed by IR spectroscopy.

[Research concerning rutin semisynthetic derivatives, synthesis and pharmaco-toxicological properties of some new morpholine and piperidine derivatives]. / Cercetari în seria derivatilor de semisinteza ai rutozidului. Sinteza si proprietatile farmaco-toxicologice ale unor noi derivati morfolinici si piperidinici.

In order to continue the research of the rutin semisynthetic derivatives we obtained some new morpholine and piperidine derivatives. Melting points, solubility, yield, C, H, N elemental analysis and UV spectra characterised all of these compounds. The toxicity was established by intraperitoneal administration at mice; the values of LD50 are between 743.75 and 856.25 mg/kg (medium toxicity). Pharmacological assays included the following parameters: leukocytes formula, NBT test, and serum complement activity. The new derivatives of rutin have a very good solubility in water, a pH closed to physiological value and immunosuppressive activity: peripheric blood PMN and lymphocytes are decreased; fagocytic capacity of peripheric blood PMN is also decreased; serum complement activity is not changed.

[Study of the cardiovascular properties of some new methyl-xanthine derivatives]. / Cercetari privind proprietatile cardiovasculare ale unor noi derivati metilxantinici.

The effects of some new methylxanthine compounds, derivatives of theophylline, theobromine and caffeine with various radicals in 8 position on blood pressure have been studied. Derivatives of theophylline (1,3-dimethyl-xanthine) with various radicals in 8 position have reduced the blood pressure. In the same experimental conditions the theobromine (3,7-dimethyl-xanthine) derivatives haven't modified the blood pressure while the caffeine (1,3,7-trimethyl-xanthine) derivatives have increased the blood pressure values.

[Xanthine derivative compounds potential activity in inflammatory process]. / Compusi cu structura xantinica potential activi în procesul inflamator.

We studied the potentially anti-inflammatory action of some new xanthine compounds, theophylline derivatives with 7-[2-hydroxy-3-(4-acetamido)-phenoxy-propyl]-8-R-1,3-dimethyl-xanthine and 8-R-1,3-bis-(1,3-dimethyl-xanthin-7yl)-2-hydroxy-propane structure substituted in 7 and 8 position. Almost all studied compounds reduced the inflammatory edema, the effect being comparable or highest theophylline. The antiinflammatory effect of theophylline intensified with the introduction in 7 position the theophylinyl radical and in 8 position the bromo, nitro, pirolidinyl, piperidinyl, morfolinyl, imidazolyl, 3,5-dimethyl-pirazolyl, 3-methyl-5-oxo-pirazolyl radicals.