A rapid practical process has been developed for synthesis of 2,4,5-trisubstituted-imidazoles in excellent yields up to 95% from readily available starting materials.
By understanding the rampant infections of Mycobacterium tuberculosis (Mtb) and inflammations caused due to the generation of radical species during the Mtb infection, a series of (E)‐2‐(2‐allylidenehydrazinyl)thiazole derivatives, with dual‐action properties, was designed. The molecules were designed with a considerable variation in LogP, one of the critical parameters in physicochemical properties, and analyzed for their drug‐likeness. For the synthesis, a simple, green, and multicomponent one‐pot synthesis method was developed. The in vitro inhibition potentials were evaluated against Mtb H37Rv by the microplate Alamar Blue assay. The results reveal that compound 6 was potent, with a MIC value of 6.5 µg/ml, and showed better interactions with the KasA protein with binding free energy (ΔG) of −9.4 kcal/mol. Also, the radical scavenging properties were studied to establish the dual‐action properties of the molecules. Compound 9 exhibited promising antioxidant and nitric oxide radical scavenging activities, with 81.7% and 81.0%, respectively, at 1,000‐μg/ml concentration.
The efficient metal-free oxidative coupling of arylmethylamines with indoles has been developed using molecular oxygen as a green oxidant towards a novel rout of 3,3′-bis(indolyl)methanes (BIMs) synthesis.
A simple copper‐catalyzed “one‐pot” process has been developed for the synthesis of poly‐substituted imidazoles. Tetrasubstituted imidazoles could be afforded in short reaction time and in excellent yields under mild and eco‐friendly conditions via direct oxidative N‐α‐C(sp3)‐H functionalization of arylmethylamines. The explored substrate scope of readily available benzylamines with 1,2‐diketones and α‐hydroxyketones has shown great utility in designing different tetrasubstituted imidazole scaffolds that are of medicinal significance through this alternative route. More information can be found in the Research Article by Vikas D. Kadu et al.
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