Design and Synthesis of Imidazo/Benzimidazo[1,2-]quinazoline Derivatives and Evaluation of Their Antimicrobial Activity.
Journal:
ACS omega
Published Date:
Nov 30, 2018
Abstract
A new class of fused quinazolines has been designed and synthesized via copper-catalyzed Ullmann type C-N coupling followed by intramolecular cross-dehydrogenative coupling reaction in moderate to good yields. The synthesized compounds were tested for in vitro antibacterial activity against three Gram negative (, , and ) and two Gram positive (, and ) bacteria. Among all tested compounds, , , and exhibited promising minimum inhibitory concentration (MIC) values (4-8 μg/mL) for all bacterial strains tested as compared to the positive control ciprofloxacin. The synthesized compounds were also evaluated for their in vitro antifungal activity against and and compounds , , and having potential antibacterial activity also showed pronounced antifungal activity (MIC values 8-16 μg/mL) against both strains. The bactericidal assay by propidium iodide and live-dead bacterial cell screening using a mixture of acridine orange/ethidium bromide (AO/Et·Br) showed considerable changes in the bacterial cell membrane, which might be the cause or consequence of cell death. Moreover, the hemolytic activity for most potent compounds (, , and ) showed their safety profile toward human blood cells.
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