RESUMEN
This paper presents the synthesis of some tetrazolium salts and metal complexes combinations, which are derived from aromatic and heterocyclic formazans. Elemental quantitative analyses and spectral data confirmed the structure of the new synthesized compounds. The new synthesized compounds were submitted to microbiological tests.
Asunto(s)
Antiinfecciosos/síntesis química , Formazáns/síntesis química , Sales de Tetrazolio/síntesis química , Antibacterianos , Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Fenómenos Químicos , Química Física , Formazáns/química , Formazáns/farmacología , Pruebas de Sensibilidad Microbiana/estadística & datos numéricos , Sales de Tetrazolio/química , Sales de Tetrazolio/farmacologíaRESUMEN
This paper presents the synthesis of six hydrazones from isatin and 1-morpholinomethyl-isatin and also of their six cooper's complex salts. Their structure was confirmed by the results of the quantitative elemental analysis and by IR, UV-VIS spectral analysis. The biological tests point out that cooper's complex salt of 3-(3'-phenyl-pyridazinylhydrazono)-5-methyl-indoline-2-one (1:2) (VI a) has the smallest toxicity (DMT over 800 mg/kg.w. p.o.), a remarkable anti-inflammatory activity (inhibition 57.1%, IAR 1.1) and also a gastroprotector coefficient of 43.3%. In the mean time, the cooper's complex salt of 3-(3'-p-anisyl-pyridazinyl-hydrazono)-5-methyl-ind oline-2-one (1:2) (VI b) has a gastroprotector coefficient of 76.3% and a lower anti-inflammatory activity than the first derivative (inhibition 36.9%).
Asunto(s)
Antiinflamatorios/síntesis química , Isatina/análogos & derivados , Piridazinas/síntesis química , Animales , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Antiinflamatorios/toxicidad , Carragenina , Evaluación Preclínica de Medicamentos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Femenino , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Isatina/química , Masculino , Ratones , Piridazinas/química , Piridazinas/uso terapéutico , Piridazinas/toxicidadRESUMEN
The paper presents a synthesis of six new Mannich bases, five hydrazones derived from 1-piperidino-methyl-5-R-isatin and three copper complex compounds of 3-(3'-R-phenyl-pyridazinil-hydrazone)-indoline-2-ones (R=H, CH3, OCH3). The structure of the new compounds was confirmed by the results of the elementary and spectral analysis. Pharmacodynamic studies indicated that copper complex compounds present effective biological properties. Thus, it can be seen that the experimental carrageenan-induced inflammatory oedema was 58.3% inhibited by the complex V (R=CH3) after oral administration. Antimicrobial tests revealed that only compound V (R=OCH3) shows a moderate antimicrobial activity against the gram-positive and gram-negative bacteria, used in the test.
Asunto(s)
Hidrazonas/farmacología , Isatina/análogos & derivados , Bases de Mannich/farmacología , Animales , Antibacterianos , Antiinfecciosos/farmacología , Antiinflamatorios/uso terapéutico , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Carragenina , Evaluación Preclínica de Medicamentos , Hidrazonas/uso terapéutico , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Isatina/farmacología , Isatina/uso terapéutico , Bases de Mannich/uso terapéutico , Ratones , Pruebas de Sensibilidad Microbiana , Relación Estructura-ActividadRESUMEN
This paper presents a synthesis about some hydrazones, formazans and copper's complexes combinations. The structure of the new compounds was confirmed by the results of the quantitative elementary and IR spectral analysis. The antimicrobial and antiinflammatory activities were investigated.
Asunto(s)
Formazáns/farmacología , Hidrazonas/farmacología , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Formazáns/síntesis química , Formazáns/química , Hidrazonas/síntesis química , Hidrazonas/química , Pruebas de Sensibilidad Microbiana/estadística & datos numéricos , Relación Estructura-ActividadRESUMEN
This paper presents the synthesis of six hydrazones obtained by treating 5-methyl-isatin or 1-morpholino methyl-5-methyl-isatin with 3-(R-phenyl)-6-hydrazino-pyridazine (R = OCH3, Cl, Br) and two complex combination with copper, derived from 3-(p-anisyl-pyridazinyl)-hydrazone-5-methyl-indoline-2- one. The structure of the new compounds was confirmed by the results of the quantitative elementary and IR, UV-VIS spectral analysis. The biological tests point out that product VI, in which a copper atom binds two molecules of 3-(p-anisyl-pyridazinyl)-hydrazono-5-methyl-indoline-2-one, has a considerable antiinflammatory activity, giving a inflammation inhibition of 39, 6%. All the synthetized compounds have a moderate antimicrobial activity against Candida albicans.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinflamatorios/síntesis química , Hidrazinas/química , Hidrazonas/síntesis química , Isatina/análogos & derivados , Piridazinas/química , Animales , Antibacterianos , Antiinfecciosos/farmacología , Antiinfecciosos/uso terapéutico , Antiinfecciosos/toxicidad , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antiinflamatorios/toxicidad , Candida albicans/efectos de los fármacos , Carragenina , Fenómenos Químicos , Química Física , Evaluación Preclínica de Medicamentos , Escherichia coli/efectos de los fármacos , Hidrazonas/farmacología , Hidrazonas/uso terapéutico , Hidrazonas/toxicidad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Isatina/química , Ratones , Staphylococcus aureus/efectos de los fármacos , Relación Estructura-ActividadRESUMEN
The conditions for obtaining and the properties of some new diazabicyclic compounds is the new step in our investigation on the benzocynoline derivatives. The structure of the new compounds was confirmed by elementary (C, H, N) and spectral analyses. The antimicrobial tests evidenced that part of the newly synthetized compounds have a good antifungal action.
Asunto(s)
Antiinfecciosos/farmacología , Fenantrolinas/farmacología , Pirazoles/farmacología , Tetrazoles/farmacología , Antibacterianos , Antiinfecciosos/química , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Fenantrolinas/química , Pirazoles/química , Relación Estructura-Actividad , Tetrazoles/químicaRESUMEN
The synthesis of eight new 1-(R-pyridazinil)-3-methyl-4-(R-phenylazo)-5-pyrazolone, the structure of which was confirmed by the results of the physicochemical analysis, is presented. The preliminary tests for determining their biological action have revealed a moderate antimicrobial activity.
Asunto(s)
Antiinfecciosos/síntesis química , Pirazoles/síntesis química , Sulfanilamidas/síntesis química , Antibacterianos , Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Fenómenos Químicos , Química Física , Pruebas de Sensibilidad Microbiana , Pirazoles/química , Pirazoles/farmacología , Piridinas/síntesis química , Piridinas/química , Piridinas/farmacología , Relación Estructura-Actividad , Sulfanilamidas/química , Sulfanilamidas/farmacología , Tiazoles/síntesis química , Tiazoles/química , Tiazoles/farmacologíaAsunto(s)
Antiinfecciosos/farmacología , Antiinflamatorios/farmacología , Piridazinas/farmacología , Animales , Antiinfecciosos/uso terapéutico , Antiinflamatorios/uso terapéutico , Evaluación Preclínica de Medicamentos , Inflamación/tratamiento farmacológico , Ratones , Pruebas de Sensibilidad Microbiana , Piridazinas/uso terapéuticoRESUMEN
By the reaction of p-bromo-phenacyl bromide on the 3,8-dimethyl- and the 3,8-di-methoxy-benzocinnoline, a cycloimmonium salts was obtained which, in the presence of triethylamine, was converted to benzocinnolinium-phenacylides. The existence in situ of the ylids was furnished evidence of the 3+2 dipolar cyclo- addition reactions with various dipolarophiles, such dimethyl and diethyl acetylenedicarboxylate, diethyl propiolate and also with diethyl azodicarboxylate. Thus, the application of the 1.3-dipolar additions is a successful route for the synthesis of some new bicyclic two nitrogen bridged systems.