RESUMEN
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.
Asunto(s)
Benceno/química , Imidazoles/química , Pirimidinas/química , Tiadiazinas/química , Tiadiazinas/farmacología , Antibacterianos/química , Antibacterianos/farmacología , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antivirales/química , Antivirales/farmacología , Benceno/farmacología , Broncodilatadores/química , Broncodilatadores/farmacología , Imidazoles/farmacología , Pruebas de Sensibilidad Microbiana , Inhibidores de Agregación Plaquetaria/química , Inhibidores de Agregación Plaquetaria/farmacología , Pirimidinas/farmacología , Espectrofotometría Infrarroja , Tiadiazinas/síntesis química , Vasodilatadores/química , Vasodilatadores/farmacologíaRESUMEN
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.
Asunto(s)
Ácido Clofíbrico/análogos & derivados , Ácido Clofíbrico/química , Hipolipemiantes/química , Rutina/análogos & derivados , Rutina/química , Enfermedades Cardiovasculares/tratamiento farmacológico , Ácido Clofíbrico/síntesis química , Humanos , Hipolipemiantes/síntesis química , Rutina/síntesis química , Solubilidad , AguaRESUMEN
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.
Asunto(s)
Xantinas/química , Broncodilatadores/química , Broncodilatadores/farmacología , Cristalización , Espectrofotometría Infrarroja , Teofilina/química , Teofilina/farmacologíaRESUMEN
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.
Asunto(s)
Bloqueadores de los Canales de Calcio/farmacología , Morfolinas/farmacología , Piperidinas/farmacología , Rutina/farmacología , Animales , Bloqueadores de los Canales de Calcio/toxicidad , Inyecciones Intraperitoneales , Linfocitos/efectos de los fármacos , Ratones , Modelos Animales , Morfolinas/toxicidad , Neutrófilos/efectos de los fármacos , Piperidinas/toxicidad , Ratas , Ratas Wistar , Rutina/toxicidadRESUMEN
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.
Asunto(s)
Presión Sanguínea/efectos de los fármacos , Cafeína/farmacología , Teofilina/farmacología , Xantinas/farmacología , Algoritmos , Animales , Estimulantes del Sistema Nervioso Central/farmacología , Ratas , Ratas Wistar , Teobromina/farmacología , Vasodilatadores/farmacologíaRESUMEN
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.