Synthesis of arylfuran derivatives as potential antibacterial agents

Bacterial infections represent a serious health care problem mainly due to the misuse and overuse of antibiotics, with consequent emergence of multidrug resistant bacterial strains. Then, because the urgent need to find novel and alternative antibacterial agents, the present work focuses on the synt...

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Bibliographic Details
Published in:	Medicinal chemistry research Vol. 30; no. 5; pp. 1074 - 1086
Main Authors:	Andrade, Marina M. S., Protti, Ícaro F., Maltarollo, Vinícius G., da Costa, Ygor F. G., de Moraes, Wesley G., Moreira, Nicole F., Garcia, Giovana G., Caran, Gabriel F., Ottoni, Flaviano M., Alves, Ricardo J., Moreira, Carolina P. S., Martins, Helen R., Alves, Maria Silvana, de Oliveira, Renata B.
Format:	Journal Article
Language:	English
Published:	New York Springer US 01-05-2021 Springer Nature B.V
Subjects:	Antibacterial activity Antibacterial agents Antibiotics Antimicrobial activity Bacteria Bioavailability Biochemistry Biomedical and Life Sciences Biomedicine Bioorganic Chemistry E coli Inorganic Chemistry Medicinal Chemistry Minimum inhibitory concentration Multidrug resistance Original Research Pharmacology/Toxicology Pseudomonas aeruginosa Synthesis Oral bioavailability Arylfuran derivatives Innovative compound Antibacterial agents
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Summary:	Bacterial infections represent a serious health care problem mainly due to the misuse and overuse of antibiotics, with consequent emergence of multidrug resistant bacterial strains. Then, because the urgent need to find novel and alternative antibacterial agents, the present work focuses on the synthesis of arylfuran derivatives with potential antimicrobial activity. Eighteen arylfuran derivatives were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus , Escherichia coli and Pseudomonas aeruginosa . Among them, seven compounds containing an amino group in their structure showed activity, with compound 24 being the most effective against both Gram-negative ( E. coli , MIC = 49 µM) and Gram-positive ( S. aureus , MIC = 98 µM) bacteria, besides having exhibited a modest activity against P. aeruginosa (MIC = 770 µM). In addition, based on in silico studies, this is a druglike compound since it does not violate any rules for predicting oral bioavailability. In this context, the significant antibacterial potential and the low similarity with known antibiotics indicate the innovative aspect of compound 24 .
ISSN:	1054-2523 1554-8120
DOI:	10.1007/s00044-021-02711-y