Ultrasound assisted, synthesis of N‐(7‐(R)‐2‐oxa‐8‐azabicyclo[4.2.0]octan‐8‐yl)isonicotinamide derivatives and their biological evaluation

Abstract

AbstractIn this study, new series of azetidine derivatives were synthesized (4a‐n) from isoniazide (1), Aromatic aldehydes (2a‐n), dihydropyran (3) using SnCl2 catalyst, via one pot multicomponent reaction/cycloaddition reaction. The synthesized azetidine derivatives were characterized by IR, 1H NMR and 13C NMR and have been screened for antimicrobial, antituberculosis and anti‐inflammatory activities. In relation to Staphylococcus aureus (ATCC 25923) promising antibacterial activity was shown, compounds 4e and 4k, followed by compounds 4h, 4n, 4f, 4g and 4l. The synthesized azetidine derivatives, 4a, 4e, 4j and 4m (with zone 12 mm) displayed antituberculosis activity. But its lower potential than, the standard streptomycin (with zone 18 mm). Further 4d compound alone displayed similar activity.