Abstract
A series of new urea derivatives, containing aryl moieties as potential antimicrobial agents, were designed, synthesized, and characterized by 1H NMR, 13C NMR, FT-IR, and LCMS spectral techniques. All newly synthesized compounds were screened in vitro against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). Variable levels of interaction were observed for these urea derivatives. However, and of major importance, many of these molecules exhibited promising growth inhibition against Acinetobacter baumannii. In particular, to our delight, the adamantyl urea adduct 3l demonstrated outstanding growth inhibition (94.5%) towards Acinetobacter baumannii. In light of this discovery, molecular docking studies were performed in order to elucidate the binding interaction mechanisms of the most active compounds, as reported herein.
Highlights
Bacterial and fungal diseases have become increasingly more prominent and complex in recent years, when compared to the last half of the twentieth century [1]
The results indicated that the adamantyl urea derivative
The structures of all synthesized compounds were confirmed by IR, 1 H NMR, 13 C NMR, and mass spectroscopic techniques
Summary
Bacterial and fungal diseases have become increasingly more prominent and complex in recent years, when compared to the last half of the twentieth century [1]. The need for new antibacterial and antifungal agents has become a goal of extreme importance, especially in light of the documented emergence of multi-drug-resistant (MDR) strains in recent years [2,3,4,5,6,7]. These MDR strains already pose a well-recognized health threat to the world population and are frequently associated with increased healthcare cost and prolonged hospital stays.
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