RESUMEN

A novel series of 3-chloro-4-[4-(2-oxo-2H-chromen-4-ylmethoxy)-phenyl]-1-phenyl-azetidin-2-one derivatives (5a-j) have been synthesized from 4-aryloxymethylcoumarins (1a-e) and 4-aryliminomethyl-phenols (3a-b). The title compounds were screened for their in vitro anti-bacterial and anti-fungal activities. Results revealed that, compounds (5c), (5f), (5h) and (5j) showed excellent anti-microbial activity against a panel of microorganisms. Brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties among which (5h) and (5j) displayed potent cytotoxic activity against Artemia salina. The DNA cleavage activity of some compounds was studied by agarose gel electrophoresis method. All synthesized compounds were characterized using IR, (1)H NMR, (13)C NMR, MS and elemental analysis.

Asunto(s)

Antibacterianos , Antifúngicos , Azetidinas/química , Diseño de Fármacos , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/síntesis química , Antifúngicos/química , Antifúngicos/farmacología , Artemia , Cumarinas/química , División del ADN/efectos de los fármacos , Electroforesis en Gel de Agar , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Estructura Molecular