Biological Significance of Ultrasound Assisted Synthesized Polycyclic Azetidine Derivatives

Abstract

Synthesized N-(7-R)-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isonicotinamide derivatives (4a-n) and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0]heptan-6-yl)isonicotinamide derivatives (5a-m) were screened for biologically activity. Both azetidine derivatives (4a-n) and (5a-m) were screened for antibacterial activity by ‘Disk Diffusion method’ using Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923) and antifungal activity using candida sp. Similar series of azetidine derivatives (4a-n) and (5a-m) were screened for in vitro antituberculosis activity by ‘Clairo Combi method’ using Mycobacterium tuberculosis and in vitro anti-inflammatory activity was evaluated using ‘HRBC membrane stabilization method’. Experimented azetidine derivatives excellent biological activities, (N-(7-R)-2-oxa-6-azabicyclo [3.2.0] heptan-6-yl) isonicotinamide derivatives (4a-n) against S. aureus bacteria and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0] heptan-6-yl) isonicotinamide derivatives (5a-m) against M. tuberculosis (T.B.). Both series of azetidine derivatives (4a-n) and (5a-m) show potent anti-inflammatory activity. All synthesized azetidine derivatives (4a-n) and (5a-m) were characterized by IR, ¹H NMR, 13C NMR and elemental analysis.

Keywords:

• Anti-inflammatory
• antituberculosis activity
• azetidine
• microbial activity

Disclosure statement

There are no conflicts of interest.