4.2 Article

Synthesis, Characterization, and Antibacterial Activity of New Isatin Derivatives

Journal

PHARMACEUTICAL CHEMISTRY JOURNAL
Volume 57, Issue 2, Pages 196-203

Publisher

SPRINGER
DOI: 10.1007/s11094-023-02867-4

Keywords

isatin; o-phenylenediamine; chemotherapeutic; amoxicillin; antimicrobial activity; antibacterial

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In this work, several Schiff base derivatives containing isatin moiety were synthesized using two methods and their antimicrobial activity was evaluated. The results demonstrated that these newly synthesized compounds exhibited strong antimicrobial activity and showed good inhibition effect.
1H-indol-2,3-dione (isatin) class of biologically active compounds have analgesic, anti-microbial, anti-inflammatory, anti-tubercular, anti-proliferative properties, and is also useful for the treatment of SARS-CoV. Schiff bases containing isatin moiety are known to have broad spectrum of biological activities like anti-viral, anti-tubercular, anti-fungal, and anti-bacterial. In this work, several Schiff base derivatives have been synthesized using two methods (synthetic and microwave) by reacting isatin with o-phenylenediamine. The synthesized compounds were structurally characterized and their in-vivo antimicrobial activity was tested against Gram-negative and Gram-positive bacteria using the inhibition zone method. Several newly synthesized isatin derivatives were found effective as antimicrobial agents and showed good potency (compounds 3c, 3d, 6a, 6b, 6d). Compound 3c displayed higher antimicrobial activity than standard drug (Amoxicillin) against Staphylococcus aureus at higher concentration (16 mu g/mL) and against Escherichia coli at lower concentration (1 mu g/mL).

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