Antibacterial efficacy of pyranopyrimidinone derivatives synthesized using a facile one-pot reaction

Discovering new and effective medications against resistant bacteria is an urgent need to save modern medicine, as well as prevent and treat life-threatening diseases. This study aimed to synthesize a series of pyrano[2,3- d ]pyrimidinone derivatives using a Tandem Knoevenagel-Michael cyclocondensation reaction. All the synthetic compounds were screened for antibacterial activity against various bacterial strains and isolates. Compound 7‐amino‐6‐cyano‐5-(5-nitrofuran-2-yl)‐pyrano[2,3 -d ]pyrimidin‐(1H,3H)-2,4‐diones ( 4s ) showed superb antibacterial activities against Staphylococcus aureus , Bacillus subtilis , and Escherichia coli with a minimum inhibitory concentration (MIC) ranging from 3.91 to 7.81 μg/mL. This compound also exhibited more potent antibacterial activity than levofloxacin against methicillin-resistant S. aureus (MRSA) with a MIC value of 3.91 μg/mL and demonstrated relatively no cytotoxicity at the mentioned MIC concentration. Field-emission scanning electron microscopy (FE-SEM) confirmed the complete damage of S . aureus and E. coli following exposure to compound 4s . The compound 4s has the potential to be used as an alternative antibacterial drug after supplementary studies.