The synthesis and antibacterial studies of polysubstituted pyrrolo[3,4‐b]pyridine derivatives have been described. The preparation of pyrrolo[3,4‐b]pyridine derivatives was carried out by the reaction of enamino imides, aromatic aldehydes and malononitrile/ethyl cyanoacetate using 10 mol % of DBU (1,8‐diazabicyclo[5.4.0]undec‐7‐ene) in ethanol at 78 °C in good yields. The compounds were characterized by standard spectroscopic techniques including IR, 1H & 13C NMR and elemental analysis and also final confirmation was done by single crystal X‐ray. The antibacterial activity of all the synthesized compounds was tested against two Gram positive (S. pneumoniae MTCC 655 and E. faecalis MTCC 439) and three Gram negative (E. coli ATCC 25922, S. typhimurium MTCC 3224, and P. aeruginosa MTCC 2453) bacterial strains. Most of the tested compounds showed moderate to good antibacterial activity. Compounds pyrrolo[3,4‐b]pyridine derivatives (4 j and 4 l) were the most potent and displayed bactericidal activities against E. coli strain with MIC (minimum inhibitory concentration) values of 62.5 μg/mL and 125.0 μg/mL respectively. Growth kinetic studies against E. coli, toxicity studies using human RBCs (red blood cells) and also docking studies of the selected compounds 4 j and 4 l supported that these compounds inhibit the growth of bacterial cells, non‐toxic in nature and interact with key amino residues of DNA (deoxyribonucleic acid) duplex (PDBID: 1BNA) and have drug‐like properties.
Nowadays, the fabrication of 2D metal−organic nanosheets (2D MONs) has entered the research arena fascinating researchers worldwide. However, a lack of efficient and facile methods has remained a bottleneck for the manufacturing of these 2D MONs. Herein, a 2D metal−organic framework (MOF), i.e., 2D Cu-MOF, was synthesized using a facile and convenient stirring method by using 4,4′-trimethylenedipyridine (TMDP) as an organic linker. The as-prepared MOF was characterized in detail and based on single crystal X-ray diffraction analysis, it was established that tangled layers in the 2D Cu-MOF are interconnected to produce thick strands. These tangled layers could be easily separated via ultrasonication-induced liquid phase exfoliation (UILPE) to give the 2D Cu-MON as illustrated through Tyndall light scattering and exhaustive microscopic exploration such as scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The application of this 2D Cu-MON was assessed in the field of drug delivery revealing exceptional drug loading for the drug lansoprazole (LPZ) by 2D Cu-MONs as well as drug release in the acidic and neutral medium demonstrating that the 2D Cu-MON is an excellent carrier for antiulcer drug delivery. For environmental protection, the application of 2D Cu-MON was also examined toward the removal of various cationic and anionic dyes with excellent selectivity toward cationic dye removal. The plausible mechanism for dye removal indicated the involvement of cation−π and π−π interactions, for the effective adsorption of cationic dyes as well as a increase in the surface area of 2D Cu-MON by UILPE. Remarkably, the high drug loading and dye removal are imputed to the increase in surface area by UILPE. In a nutshell, the developed 2D Cu-MON will prove to be beneficial for application in the field of drug delivery as well as for wastewater treatment.
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