Synthesis and evaluation of antibacterial and antifungal activity of new series of thiadiazoloquinazolinone derivatives. | ||
| Egyptian Journal of Chemistry | ||
| Article 67, Volume 65, Issue 5, May 2022, Pages 711-722 PDF (368.89 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2021.97638.4557 | ||
| Authors | ||
| Aly Aly* 1; Abdelmotaal Abdelmajeid2; Eman M Zahran2 | ||
| 1Chemistry Department, Faculty of Science, Benha University, Benha, Egypt | ||
| 2Chemistry Department, Faculty of Science, Benha University, Benha, Egypt. | ||
| Abstract | ||
| A facile and convenient synthesis of 1,3,4-thiadiazolyl quinazolinone derivatives is described via cyclization of anthranilic acid with maleic anhydride, which upon reaction with glycine afforded 3-glycinyl quinazolinone derivative (2), then treated with thiosemicarbazide and produced 1,3,4-thiadiazolyl quinazolinone derivative (3). Moreover, benzoxazinone isothiocyanate (13) is used as a key compound in synthesizing of triazolyl-(14), oxazolidinyl-(15) and triazinanyl-(16a,b) benzoxazinone heterocycles by reaction with phenyl hydrazine, glycine and urea and/ or thiourea, respectively. Evaluation of antimicrobial activity of some of the synthesized compounds against selected bacteria and fungi strains in comparison with Ampicillin as antibacterial agent and Amphotericin B as antifungal agent exhibited promising activity as compared to the references. The structures of the synthesized compounds were confirmed on the basis of their elemental analyses as well as spectral data (IR, MS and 1H NMR). | ||
| Keywords | ||
| N-heterocycles; thiadiazolylquinazolinones; isothiocyanato benzoxazinone; antibacterial activity; antifungal activity | ||
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