No abstract

The paper describes the synthesis, characterization data, and biological activity (antibacterial, antifungal, and brine shrimps lethality) of new azetidin‐2‐ones. The compounds have been synthesized by the reaction of diarylketenes, generated in situ from thermal decomposition of the 2‐diazo‐1,2‐diarylethanones, with N‐(1‐methyl‐1H‐indol‐3‐yl)methyleneamines. The compounds have been characterized by elemental analysis and spectral (IR, 1H and 13C NMR, and MS) data. The paper also reports the results of antibacterial, antifungal, and brine shrimps lethality assays of these compounds. Some of the compounds exhibited significant biological activity.

The present paper reports an easy preparation of imines of N-methyl-1H-indole-3-carboxaldehyde by its condensation with alkyl and aromatic amines in ethanol without using any catalyst or dehydrating agent. The compounds have been screened for their antibacterial, antifungal, crown gall tumor inhibitory, and cytotoxic activities. As a major finding some of the compounds exhibited potential biological activity. The imine containing a 4-chlorophenyl group exhibits potential antitumor activity and brine shrimp lethality against crown gall tumor and brine shrimps, respectively. Furthermore, this imine containing a 4-chlorophenyl group also exhibits significant antifungal activity against Candida albicans fungal strains. The compound containing N-diphenylmethyl group has been observed most active against the Gram-positive bacteria.

Novel azetidine‐2‐ones (III), obtained via Staudinger cycloaddition, are screened for their antileishmanial activity against Leishmania major.