ANTIMICROBIAL POTENTIAL OF NOVEL BENZOXAZINONE DERIVATIVES TETHERED WITH THIOSEMICARBAZONE SCAFFOLD Authors: Mandru P*And Parameshwar P
ABSTRACT
Versatile biological activity profile of the benzoxazinone scaffold attracted the medicinal
chemists to explore lead molecules for the treatment of various microbial diseases. Extended
literature avowed the indisputable antimicrobial properties of thiosemicarbazones that
stimulated us to the current exploration. Synthesis of novel benzoxazinonethiosemicarbazone (5a-5c) hybrids from the condensation of substituted anthranilic acid (1a1c), with acetyl chloride (2) to methyl bzoxazine-4-ones (3a-3c) that are oxidized using
selenium dioxide to the corresponding aldehydes(4a-4c) followed by the condensation with
various thiosemicarbazides. Fifteen novel benzoxazinone-thiosemicarbazone (5a1-5a5, 5b1-
5b5&5c1-5c5) were synthesized in adequate yields and characterization of the molecules was
done by detailed spectral analysis using advanced analytical support. The titled compounds
were screened for antibacterial and antifungal activities. Results proclaimed that all the
synthesized compounds were exhibiting antimicrobial properties. Compound5b4 was
contended to bear potent antimicrobial properties against the given bacterial and fungal
strains.
Keywords: Benzoxazin-4-one, Thiosemicarbazone, Antibacterial, Antifungal, Agar disc
diffusion Publication date: 01/11/2022 https://ijbpas.com/pdf/2022/November/MS_IJBPAS_2022_6109.pdfDownload PDFhttps://doi.org/10.31032/IJBPAS/2022/11.11.6109