RESUMEN
Aminoalkyl derivatives of diarylmethanes were prepared using Grignard, Friedel-Crafts arylation and aminohydrochloride chain formation reactions. These series of compounds were evaluated against Mycobacterium tuberculosis H(37)R(v) and showed the activity in the range of 6.25-25 microg/mL. Effect of heteroaryl, anthracenyl and phenanthrene groups on diarylmethane pharmacophores for antitubercular activity is described.
Asunto(s)
Antituberculosos/síntesis química , Antituberculosos/farmacología , Metano/análogos & derivados , Metano/síntesis química , Metano/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Animales , Línea Celular Tumoral , Chlorocebus aethiops , Ensayos de Selección de Medicamentos Antitumorales , Indicadores y Reactivos , Macrófagos/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Ratones , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja , Relación Estructura-Actividad , Células VeroRESUMEN
A new series of diarylmethylnapthyloxy ethylamines were synthesized by aminoalkylation of diarylmethylnaphthols which were obtained by Friedel-Crafts alkylation on 1- and 2-naphthols using diarylcarbinols as the alkylating agents. The title compounds were evaluated for antitubercular activity against Mycobacterium tuberculosis H(37)R(v) in vitro and showed MIC in the range of 3.12-25 microg/ml.