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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
Meshram et al. synthesized [52] N-thiazole-3-phenyl-4-aryl-azetidin-2-ones (6) from 2-aminothiazole following the ketene-imine cycloaddition methodology in dioxane in the presence of an organic base (triethylamine). Both the microwave-assisted (85–95% yield, 1.5–2 min) as well as the classical procedure (oil bath, 62–65% yield, 8–10 h) were studied. The antibacterial activity of eight newly synthesized monocyclic β-lactam derivatives (6) was screened against two Gram-positive (Staphylococcus aureus and Proteus vulgaris) and two Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. The compounds showed good activity against all the four strains. It was hypothesized that the presence of more than one pharmacophore site (including β-lactam) was responsible for good antibacterial activity. The difference in charges between two heteroatoms of the same pharmacophore site might facilitate the inhibition of bacteria, more than viruses (Scheme 10.3).
Synthesis, spectral-characterization, biological and DFT studies of mixed ligand metal(II) complexes of 1,10-phenanthroline bearing 2-aminothiazole moiety
Published in Inorganic and Nano-Metal Chemistry, 2020
Chellaian Justin Dhanaraj, Dharmasingh Sobhanabai Remya
The interesting invention of Schiff base ligand provides an array of valuable advantages in the study of coordination metal(II) chemistry through transition metal complexes. The L together with [CoLphen], [NiLphen], [CuLphen] and also [ZnLphen] having S, O, N donor atoms, show excellent stereochemical, electronic and electrochemical properties.[1] Schiff bases of mixed ligand complexes are produced by the condensation of aldehydes and amines/ketones, as a result, they form azomethine (>C=N) bond. Mainly Schiff bases with azomethine linkage are fundamental for various biological applications in the field of antitumor, antioxidant, catalysts, antifungal and antibacterial activity.[2–5] Compounds containing aminothiazole derivatives have potent biological applications in the path of the anti-inflammatory, anticancer, antitumor, antihypertensive, antidiabetic, antileishmanial, neuroprotective, and antiviral agent, DNA binding and cleavage, antituberculosis and in therapeutic fields.[6–8] Researchers discovered that the mixed ligand metal(II) complexes medicinally act as an exponent DNA-target substance for antiviral and anticancer treatment.