RESUMEN
Porphyromonas gingivalis is a major etiologic agent and a key pathogen responsible for the development and progression of chronic periodontitis. Controlling the number of periodontal pathogens is one of the primary actions for maintaining oral health; therefore, active compounds with a capacity to exert antimicrobial activity have received considerable attention as they may represent potential new therapeutic agents for the treatment of chronic periodontitis. Heterocyclic compounds possessing 1,2,4- or 1,2,3-triazoles are known for several biological activities, including antibacterial properties. Among them are stable hemiaminals which can be obtained in reaction between nitrobenzaldehyde derivatives and 4-amino-1,2,4-triazole or 4-amino-3,5-dimethyl-1,2,4-triazole. In this study, we selected two relatively stable hemiaminals: (2,4-dinitrophenyl)(4H-1,2,4-triazole-4-ylamino)methanol (24DNTAM) and (2,4-dinitrophenyl)(4H-3,5-dimethyl-1,2,4-triazole-4-ylamino)methanol (24DNDMTAM). Both compounds showed promising anti-P. gingivalis activity, higher against ATCC 33277 strain as compared to A7436 strain. The lowest hemiaminal concentration inhibiting visible planktonic bacterial growth under high-iron/heme conditions was â¼0.06 mg/ml, and the lowest hemiaminal concentration showing killing of bacteria was â¼0.25 mg/ml. Antimicrobial activity was also observed against P. gingivalis grown on blood agar plates. Slightly higher antimicrobial activity of both compounds was observed when P. gingivalis was grown in co-cultures with epithelial HeLa cells under low-iron/heme conditions, which mimic those occurring in vivo. 24DNTAM was more effective against P. gingivalis, but exhibited higher cytotoxic activity against epithelial and red blood cells, as compared with 24DNDMTAM. We conclude that both hemiaminals might originate a novel group of biologically important molecules.
Asunto(s)
Antibacterianos/farmacología , Porphyromonas gingivalis/efectos de los fármacos , Triazoles/farmacología , Antibacterianos/síntesis química , Técnicas de Cocultivo , Células Epiteliales/microbiología , Células Epiteliales/fisiología , Células HeLa , Humanos , Pruebas de Sensibilidad Microbiana , Viabilidad Microbiana/efectos de los fármacos , Modelos Moleculares , Estructura Molecular , Porphyromonas gingivalis/crecimiento & desarrollo , Triazoles/síntesis químicaRESUMEN
Studies on the stable hemiaminals and Schiff bases formation in the reaction of substituted benzaldehydes with primary 3,5-dimethyl-1,2,4-triazole 4-amine were carried out under neutral conditions. These products were investigated by IR, Raman, MS, ¹H- and (13)C-NMR spectra as well as by X-ray crystallography. The effect of reaction conditions: temperature, polarity of the solvents utilized, substrate concentration and the ortho and para benzaldehyde substituents on the yield of products was also examined.
Asunto(s)
Aminas/química , Benzaldehídos/química , Triazoles/química , Cristalografía por Rayos X , Estructura Molecular , Bases de SchiffRESUMEN
Stress cardiomyopathy is an acute transient left ventricular dysfunction, associated with emotional stress. In the course of alcohol withdrawal abnormalities of perfusion and myocardial contractility have been described, manifested in the scintigraphic study, with the absence of changes in ECG and echocardiography and probably caused by sympathicotony, in analogy to severe emotional stress. We present a case of acute left ventricular dysfunction during alcohol withdrawal with significant changes in echocardiography and ECG mimicking acute coronary syndrome. In a 53-year-old woman, treated in the internal ward because of abdominal pain, vomiting, and moderately elevated pancreatic amylase in serum and urine, chest pain and shortness of breath at rest occurred during the first day of hospitalization. These symptoms were accompanied by ST segment elevation in V2-V3, negative T waves in V2-V6 and an increase in troponin. Coronarography excluded significant changes in the arteries, the echocardiography revealed apical akinesis with left ventricular ejection fraction (LVEF) 30%. By hospital day 3 disorientation and behavior disorders corresponding of alcohol withdrawal appeared. In subsequent days improvement in LV systolic function was observed with LVEF increase to 53%. ECG changes in the form of a deep negative T waves in I, II, aVL and V2-V6 persisted to the end of hospitalization.