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.
An efficient multicomponent approach has been developed in the environmentally green aqueous medium for synthesis of substituted polyfunctionalized pyrazoles. The simple and readily available aldehydes, malononitrile and phenylhydrazines substrates afforded polysubstituted imidazoles (15 examples) up to 96 % yield. The polyethylene glycol is playing the dual role of solvent and promoter with water in this reaction catalyzed by ceric ammonium nitrate.
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