Design, Synthesis, and Biological Evaluation of Melatonin-Coumarin Hybrids as Potential Antibacterial Agents
Martinez, Deziray A.
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The discovery of antibiotics in the 20th Century markedly reduced the threat of infectious diseases across the globe, but use of these medicines has unfortunately resulted in the natural selection of antibiotic-resistant strains of bacteria. Accompanied by this is an increasing number of antibiotics that are becoming ineffective against many fatal bacterial infections; the development of novel antibiotics would thus provide significant health benefits. Two molecules that have previously demonstrated promising antibacterial activity according to scientific literature are melatonin and coumarin. It was particularly observed that coumarin derivatives with substituents at C-7 are effective at inhibiting the growth of various bacterial species. The synthesis of eight melatonin-coumarin hybrids as potential antibacterial agents was therefore undertaken via molecular hybridization (MH), with emphasis placed on the role of C-7 substituents in producing antibacterial activity. Theoretically, MH would work especially well in the design of antibiotics as MH produces multi-target compounds which would reduce the development of resistance. Subsequent biological evaluation against Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Escherichia coli demonstrated an absence of antibacterial activity by all compounds.