RESUMEN
Tuberculosis treatment remains a challenge that requires new antitubercular agents due to the emergence of multidrug-resistant Mycobacterium strains. This paper describes the synthesis, the antitubercular activity and the theoretical analysis of N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides (8a-b, 8e-f, 8i-j and 8n-o) and new analogues (8c-d, 8g-h, 8l-m and 8p-q). These derivatives were synthesized in good yields and some of them showed a promising antitubercular profile. Interestingly the N-acylhydrazone (NAH) 8n was the most potent against the Mycobacterium tuberculosis H37Rv strain (MIC=2.5 µg/mL) similar to or better than the current drugs on the market. The theoretical structure-activity relationship study suggested that the presence of the furyl ring and the electronegative group (NO(2)) as well as low lipophilicity and small volume group at R position are important structural features for the antitubercular profile of these molecules. NMR spectra, IR spectra and elemental analyses of these substances are reported.
Asunto(s)
Antituberculosos/síntesis química , Antituberculosos/farmacología , Hidrazinas/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Triazoles/química , Antituberculosos/química , Relación Dosis-Respuesta a Droga , Hidrazinas/síntesis química , Hidrazinas/química , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Estructura Molecular , Estereoisomerismo , Relación Estructura-ActividadRESUMEN
This paper describes the synthesis, antiplatelet and theoretical evaluations of 10 N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides (2a-j). These compounds were synthesized, characterized and screened for their in vitro antiplatelet profile against human platelet aggregation using arachidonic acid, adrenaline and ADP as agonists. Among NAH derivatives 2a-j, the compounds 2a, 2c, 2e, 2g and 2h were the most promising molecules with significant antiplatelet activity.
Asunto(s)
Hidrazinas/síntesis química , Inhibidores de Agregación Plaquetaria/síntesis química , Triazoles/síntesis química , Humanos , Hidrazinas/química , Hidrazinas/farmacología , Agregación Plaquetaria/efectos de los fármacos , Inhibidores de Agregación Plaquetaria/química , Inhibidores de Agregación Plaquetaria/farmacología , Relación Estructura-Actividad , Triazoles/química , Triazoles/farmacologíaRESUMEN
This paper describes the antiviral evaluation of new N-amino-1,2,3-triazole derivatives, 1-(substituted-phenylamino)-5-methyl-1H-[1,2,3]-triazole-4-carboxylic acid ethyl esters, 3 and 1-(4-substituted-phenylamino)-5-methyl-1H-[1,2,3]-triazole-4-carboxylic acid hydrazides, 4, on Cantagalo virus replication. 1-(4-Fluoro-phenylamino)-5-methyl-1H-[1,2,3]-triazole-4-carboxylic acid hydrazide, 4e, exhibited a significant antiviral effect. Characterization of all compounds was confirmed by IR, (1)H and (13)C spectroscopies and elemental analysis. In addition, molecular structure of 4e was also reported.
Asunto(s)
Amitrol (Herbicida)/análogos & derivados , Amitrol (Herbicida)/farmacología , Antivirales/química , Antivirales/farmacología , Virus Vaccinia/efectos de los fármacos , Amitrol (Herbicida)/toxicidad , Animales , Antivirales/toxicidad , Línea Celular , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad , Proteínas Virales/análisis , Proteínas Virales/metabolismoRESUMEN
The efficiency of a commercial peracetic acid sanitizer on destruction of Staphylococcus aureus and Escherichia coli was evaluated using two distinct methods. The first method is the AOAC suspension test and the second is a method proposed by one of the authors in which the microbial cells are settled on a stainless steel surface and then treated with the sanitizer. The results showed that when in suspension S. aureus was more resistant to the sanitizer than E. coli. When S. aureus was settled on the stainless steel surface, the contact time between the sanitizer and the microorganisms to attain a 6.5 log reduction in the number of viable cells was three times greater than when the cells were in suspension.