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In this study, a series of 1,3,4-thiadiazole-thiazolidinone derivatives (7a–j) were synthesized as carbonic anhydrase inhibitors. The in vitro carbonic anhydrase inhibitory activity of these synthesized compounds was determined and the results revealed that compound 7i (IC50 = 0.402 ± 0.017 μM) is more potent than the standard reference acetazolamide (IC50 = 0.998 ± 0.046 μM). Moreover, kinetic analysis was also performed to see the mode of binding with the target enzyme, and it was shown that compound 7i bound with the target in a competitive manner. All compounds were screened for antioxidant activity against DPPH and anticancer activity against A549 (human lung cancer cells), and the MTT assay results indicated that compounds 7a and 7d had more inhibitory growth. Moreover, compound 7i exhibited a good conformational state with hydrogen bond interactions within the receptor binding pocket according to molecular docking studies. Therefore, the novel compound 7i might be employed as a promising pharmacophore for potent and selective carbonic anhydrase inhibitors. [ABSTRACT FROM AUTHOR]

In the present work, iron oxide nanoparticles (Fe3O4-NPs) were prepared using a chemical coprecipitation method. At room temperature, Fe3O4-NPs are put in interlamellar space and external surfaces of montmorillonite (MMT) as a supported solid. The MMT@Fe3O4 was characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), vibrating sample magnetometer (VSM), thermogravimetric analysis (TGA) and Fourier transform infrared spectrophotometry (FT-IR). Then, indeno[1,2-b]indolone derivatives were catalyzed by magnetic MMT@Fe3O4-NPs. MMT@Fe3O4-NPs were found to be a recoverable organocatalyst for the effective synthesis of the indeno[1,2-b]indolone derivatives via one-pot multicomponent cyclocondensation of ninhydrin, 1,3-diketo compound and amine derivatives in water. The significant advantages of this method are excellent yield, mild conditions, eco-friendly catalyst, low expense, and not using an environmentally harmful catalyst or solvent. [ABSTRACT FROM AUTHOR]

A practical and simple approach for the one‐pot multicomponent synthesis of indenopyrazolones is described via the condensation of ninhydrin (indan‐1,2,3‐trione), phenylhydrazine, and various aldehydes in the presence of MMT@Fe3O4 as an environmentally benign core/shell nanocomposite catalyst. The catalyst could be recycled using an external magnet easily and reused several times without remarkable loss of its catalytic activity. Furthermore, avoiding hazardous solvents, reusability of the catalyst, easy work‐up, short reaction times, room temperature, and mild reaction conditions are the advantages of this new eco‐friendly protocol. [ABSTRACT FROM AUTHOR]