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New candidates of N-phenylpyrazoline derivatives were designed combining the Indole moiety to explore its potential as antimicrobial and antioxidant activity. The starting material synthesis was achieved through One-pot three-component reaction; at that point, it was acylated and interacted with various substituted benzaldehydes to result in new chalcones that were later cyclized to N-phenylpyrazoline, through reaction with phenyl hydrazine. The structures of the synthesized compounds were reinforced by their spectral data. The final compounds were screened for antibacterial activity against resistant strains of Staphylococcus aureus and Escherichia coli microorganisms; as a result, it showed that the compounds with methoxy group at position meta and hydroxy at position ortho were the highly active derivatives. Meanwhile, the highly active compound with antifungal activity against C. Albicans, had nitro group at para position. During the evaluation of proton donating antioxidant activity, using DPPH radical scavenging assays method; it was exposed that, the derivatives with highly active antibacterial had the most antioxidant activity. In the final step, the molecular docking study exposed that the compound with highly active antibacterial and antioxidant activity was the most potent derivative. The resulting studies disclosed that the synthesized N-phenylpyrazoline derivatives displayed less specificity than the reference compounds.

Four membered cyclic amides that are a broadly utilized class of antimicrobial agents up to now. Moreover, Symmetrical Bis-Schiff bases constitute an extraordinary class of strained compounds with varied applications and building blocks for the synthesis of 2-Azetidinones antibiotics. Because of those over biological significance, this study concludes a versatile synthetic precursor for the synthesis of the new Symmetrical Bis-Schiff bases and 2-Azetidinones in an exceedingly high yield. 2-Azetidinones were synthesized through [2+2] dichloroketene-imine cycloaddition reaction. The structures of the synthesized compounds were characterized by FT-IR, 1H-NMR, and 13C-NMR. Additionally, the products were assayed against two antibacterial types Gram-positive (S. aureus) and Gram-negative (E. coli) microorganisms and two varieties of fungal strains A. niger, T. mentagrophytes by broth microdilution method. As a result, all synthesized compounds displayed good antimicrobial activities against resistant strains. Finally, molecular docking studies were explained the inhibitory activities for the new products with the target (PDB ID: 1MWU) methicillin acyl-Penicillin binding protein 2a from methicillin-resistant Staphylococcus aureus strain 27r at 2.60 Å resolution.

This study illustrates the synthesis and spectroscopic study of new β-lactam and novel Pyrrolone derivatives with the study of their antioxidant and antibacterial activities. This study included two major steps, the first step involved the synthesis of imine derivatives (3a-j) from sulfadiazine. The second step contained the synthesis of 2-Azetidinone (4a-j) and Pyrrolone (5a-j) heterocyclic compounds that have been generated through the reaction between synthesized imine derivatives with chloroacetyl chloride and fumaryl chloride in the presence of triethylamine, respectively. The structures of the synthesized compounds were confirmed on the basis of their spectral data such as FT-IR, 1H-NMR and 13C-NMR spectra, which provided the expected frequencies and signals. Lastly, all products were screened for the antioxidant activity and against two kinds of bacteria Staphylococcus aureus G (+ve) and Escherichia coli G (-ve) microorganisms. The products showed lower to high antioxidant activity as compared to standard ascorbic acid. Some of the products evaluated inactive and others slight to high activity against both kinds of bacteria.

The present study deals with the synthesis, spectroscopic characterization, antibacterial and antifungal activities of novel series five-membered ring heterocyclic compounds containing nitrogen and sulfur heteroatoms. The synthetic routes have been divided into two parts: The first one includes synthesis of compounds (4a-c) through one pot operation three component reaction of 2-naphthol (1), substituted benzaldehyde (2a-c) and thiourea (3) in 1,2-dichloromethane, using a catalytic amount of ZrOCl2.8H2O and compound (6) was synthesized using semicarbazide (5) in absolute ethanol and indium (III) chloride as catalyst. The second part is the hetero-cyclization reactions of the compounds (4a-c and 6) to obtain the heterocyclic compounds (7a-c, 8, and 9). The structures of the synthesized products are verified on the basis of (FT-IR, 1H-NMR and 13C-NMR) spectroscopy. The synthesized compounds antibacterial activities were screened against Staphylococcus aureus (Gram positive) and Escherichia coli (Gram negative) bacteria as compared to standard amikacin and antifungal activity against Candida albicans fungi as compared to standard Nystatin, well diffusion method is used. The antibacterial and antifungal activities of synthesized compounds (7a-c, 8 and 9) were higher than the antibacterial and antifungal activities of synthesized compounds (4a-c and 6).