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Microwaves in Lactam Chemistry
Published in Banik Bimal Krishna, Bandyopadhyay Debasish, Advances in Microwave Chemistry, 2018
Dr. Debasish Bandyopadhyay, Bimal Krishna Banik
Microwave-assisted synthesis of the compounds (66a–67d) was carried out through 1,3-dipolar cycloaddition of isatin, 1,3-thiazole-4-carboxylic acid, and a Knoevenagel adduct in 2,2,2-trifluoroethanol as a green solvent. All four compounds demonstrated high antibacterial activity against Klebsiella pneumonia with MIC value ranging from 0.005 to 0.19 µg/mL. In addition, the compound 67c exhibited in silico drugability against the protein New Delhi Metallo-beta-Lactamase-1 (NDM-1; PDB ID: 4HL2) [107].
Structural effects of nanoparticles on their antibacterial activity against multi-drug resistance
Published in Inorganic and Nano-Metal Chemistry, 2022
Bharti Goyal, Neelam Verma, Tannu Kharewal, Anjum Gahlaut, Vikas Hooda
Over the recent years, the bacterial community has developed antibiotic-resistant strains (mainly MDR strains) that can confront the given mode of action of antibiotics. They have accomplished various resistance strategies. These include—the expression of genes that promote the efflux of antibiotics,[3] the synthesis of an enzyme that can degrade or alter antimicrobial agents,[4] modification of cellular components such as cell walls, ribosomes.[5] Clinically, due to misuse of antibiotics, “superbugs” have been reported which are almost resistant to all antibiotics.[3] They are supposed to contain a gene named—New Delhi Metallo-beta-lactamase 1 (NDM-1).[6] Most of the bacteria aggregate by extracellular polymeric substance (EPS) and form biofilm. It acts as a fence and blocks the entry of antibiotics, offers a basis for prolonged infections.
Antimicrobial efficiency of diorganotin(IV) bis-[3-(4-chlorophenyl)-2-methylacrylate]
Published in Journal of Coordination Chemistry, 2018
Niaz Muhammad, Naseer Ali Shah, Saqib Ali, Abdul Wadood, Mehreen Ghufran, Muhammad Rashid Khan, Pakiza Siddiq, Shaukat Shujah, Auke Meetsma
To specify the target for the antibacterial and antifungal activities of the synthesized complexes, 1 was selected as the model compound for its higher antimicrobial efficiency among the synthesized complexes. Sixteen different target proteins that is, six target proteins were selected as fungal (Aspergillus flavus, Aspergillus niger, and Aspergillus fumigates) targets while ten targets for bacterial strains (Staphylococcus aureus, Micrococcus luteus, Enterobacter aerogenes, Klebsiella pneumonie, Escherichia coli, and Bordetella bronchiseptica) were obtained from the Protein Data Bank. Among these 16 target proteins, only the two target proteins, that is, deglycating enzyme fructosamine oxidase from Aspergillus fumigatus and New Delhi metallo-beta-lactamase-1 from Klebsiella pneumonia were preferred as they showed good interactions and binding energies with the synthesized complex in the docking simulation by MOE 2016.08 [29], while the others have less binding energies and interactions as well as binding pockets that are too small to fit the large complex. Fungal fructosamine oxidases are peroxisomal enzymes that catalyze oxidation of the C-N bond between the nitrogen of the amino portion of the fructosamines and C1 of the fructosyl moiety. On the other hand New Delhi metallo-beta-lactamase-1 is a class B beta-lactamase and can hydrolyze all beta-lactam antimicrobials, therefore, most New Delhi metallo-beta-lactamase-1 positive bacteria are resistant to a wide variety of antimicrobial agents. Before the docking studies, the structure of the synthesized complex was built and saved in its 3D conformation by MOE 2016.08. The drug targets were downloaded with a high resolution and without a mutation or missing residues around the active site. The ligands, oligomeric chains, water molecules or solvent were removed from the proteins. The energies of the protein molecules were minimized after the 3D protonation using the default parameters of MOE (Molecular Operating Environment) software (www.chemcomp.com) energy minimization algorithm (gradient: 0.05, Force Field: MMFF94x).