Design, synthesis and biological evaluation of some novel isoniazid cyclocondensed azetidinones

Abstract

Background

In the present study, a series of novel azetidinone derivatives synthesized because of its potent antimicrobial and antimycobacterial activity.

Method

Compounds (10a–10j) were synthesized by reacting Schiff's base of isoniazid reacted with, chloro acetyl chloride in presence of triethyl amine and 1, 4-dioxane as an efficient catalyst, analyzed for their structures. in vitro antimicrobial and antimycobacterial activity were carried out.

Results

Among the synthesized compounds, compound 10b and 10i was found to be the most potent against gram-positive bacteria Bacillus subtilis, gram-negative bacteria Escherichia coli, Mycobacterium tuberculosis CIP and M. tuberculosis H37Rv.

Conclusion

A series of novel azetidinone derivatives of biological interest were synthesized and analyzed, suggests that it an interesting compound compared to the current therapeutic agents and are considered to investigate further for the same.