Abstract
A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthesized chalcones were established by IR and 1H-NMR analysis. The biological data shows that compounds p5, f6 and t5 had strong activities against both susceptible and resistant Staphylococcus aureus strains, but not activity against a vancomycin and methicillin resistant Staphylococcus aureus isolated from a human sample. The structure and activity relationships confirmed that compounds f5, f6 and t5 are potential candidates for future drug discovery and development.
Highlights
Many decades since penicillin was discovered and introduced as a powerful antibacterial agent, antibiotics have become critical in the fight against infectious diseases caused by bacteria and other microbes
Widespread antibiotic use has promoted the emergence of antibiotic-resistant pathogens, including multidrug resistant strains [1,2,3]
A number of known and novel heterocyclic chalcone analogues were prepared via Claisen Schmidt condensation reactions [14,30] between appropriate benzaldehydes and heteroaryl methyl ketones like pyridine-2-yl methyl ketone, thiophene-2-yl methyl ketone and furan-2-yl methyl ketone (Scheme 1)
Summary
Many decades since penicillin was discovered and introduced as a powerful antibacterial agent, antibiotics have become critical in the fight against infectious diseases caused by bacteria and other microbes. The appearance of more and more pathogenetic bacterial species resistant to conventional antibiotics has resulted in either high expenses or failure in the treatment of infectious diseases. An alarming increase in resistance of bacteria that cause community acquired infections has been documented, especially in Staphylococci and Pneumococci, which are prevalent causes of disease and mortality. With the emergence of new microbial strains resistant to many conventional available antibiotics there is growing interest in the discovery of new antibacterial agents [1,2]. According to the known structure and activity relationships, it is considered that certain small heterocyclic molecules act as highly functionalized scaffolds and are known pharmacophores of a number of biologically active and medicinally useful molecules [5,6]
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