RESUMEN
BACKGROUND: Herein, a new chitosan-supported ytterbium nano-catalyst has been prepared and used in a mild, efficient, and expeditious method for the synthesis of substituted piperidine derivatives via threecomponent condensation of substituted anilines, formaldehyde and different cyclic/acyclic active methylene compounds at room temperature. METHODS: The catalyst was characterized by FTIR, XRD, SEM, EDX, TEM, ICP-AES and the stability of the catalyst was evaluated by TG analysis. The synthesized compound 3,3,11,11-Tetramethyl-15-(phenyl)-15- azadispiro[5.1.5.3]hexadecane-1,5,9,13-tetrone (3a) was explored for pBR322 DNA cleavage activity and genotoxicity. Further, the interaction of 3a with CT-DNA was investigated through UV-vis, fluorescence and viscosity. RESULTS: The preparation of Yb/chitosan nano-catalyst was verified and the catalyst was found effective towards substituted piperidine formations with the catalyst reusability. Compound 3a was successfully tested for DNA cleavage activity. In addition, fluorescence results revealed that compound 3a interacted with DNA with a binding affinity of 4.84 x 104 M-1. CONCLUSION: Our findings suggest that compounds bearing spiro-piperidine scaffold, synthesized using reusable nano-catalyst, could be effective biological agents.
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Quitosano , Catálisis , ADN , Humanos , Piperidinas , ViscosidadRESUMEN
Waste biomass derived heterogeneous catalyst is an excellent alternative to chemically synthesized catalysts. In this work, calcined Tectona grandis leaves were proposed as an eco-friendly, renewable and low cost heterogeneous base catalyst. The prepared catalyst was examined by FTIR, XRD, XPS, SEM, EDX, TEM, TGA, BET and Hammett indicator test. The catalyst has an appealing nature towards various chemical transformations due to its basic surface sites provided by alkali and alkaline earth metals. The efficiency of the catalyst was successfully investigated by its application in biodiesel production. The products were confirmed by 1H and 13C NMR. 100% FAME conversion was attained using a catalyst loading of 2.5â¯wt% under optimized reaction parameters. The catalyst was further explored for Knoevenagel condensation reaction, in which it showed its effectiveness and recyclability towards the formation of benzylidenemalononitrile derivatives of aryl aldehydes. Thus, it is a potential 'green catalyst' derived from waste biomass without any addition of chemicals that can replace the industrial base catalysts used for biodiesel production and Knoevenagel reaction and makes the protocol environmentally benign.
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Biocombustibles , Hojas de la Planta , Catálisis , EsterificaciónRESUMEN
Fatty acid functionalized chitosan conjugates are of great interest in cancer therapeutics because of its internalization through receptor mediated endocytosis into the cancer cells. Keeping the above fact into consideration, herein we synthesized the undec-10-enoic acid functionalized chitosan based undecyl-chitosan (U-CS) nano-bioconjugate with the use of DCC as a coupling agent. The U-CS conjugate synthesized was confirmed and characterized by FTIR, 1H NMR, TGA, XRD, SEM and TEM analysis. Generally, it is well established that conjugates of oleic acid with human Alpha-lactalbumin (HAMLET) induce cytotoxicity in the altered cells, but not in healthy cells. To check our presumptions, anti-bacterial and anti-cancer potential of U-CS was evaluated against bacterial pathogens (Gram +ve and Gram -ve) and human cancer cell lines (HeLa, MDA-MB-231 and Hep3B). The results of our study clearly revealed that conjugate showed enhance anti-bacterial, anti-biofilm as well as anti-cancer efficacy as compared to pure and free form of the chitosan.
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Antibacterianos/farmacología , Antineoplásicos/farmacología , Biopelículas/efectos de los fármacos , Quitosano/química , Nanoconjugados , Ácidos Undecilénicos/química , Bacterias , Línea Celular Tumoral , Humanos , Lactalbúmina , Ácido OléicoRESUMEN
An efficient synthesis of fatty acid derivatives of 1,3,4-oxadiazole has been reported and comparative study between conventional heating to that of microwave irradiation also described. The newly synthesized compounds (2A-F) were characterized by FT-IR, (1)H NMR, (13)C NMR and mass spectral analysis. The binding interaction of (Z)-2-(heptadec-8'-enyl)-5-methyl-1,3,4-oxadiazole (2C) with human serum albumin (HSA) has been evaluated by UV, fluorescence, circular dichroism (CD) and molecular docking studies. Fluorescence results showed that compound 2C interacts with HSA through static quenching mechanism with binding affinity of 2 × 10(3) M(-1) and Gibbs free energy change (ΔG) was found to be -16.83 kJ mol(-1). Molecular docking studies have been performed to evaluate possible mode of interaction of compound 2C with HSA.