Journal
FRONTIERS IN CHEMISTRY
Volume 7, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fchem.2019.00475
Keywords
antibiotics; drugs; isocyanides; multicomponent reactions; resistant bacteria
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Funding
- Ministerio de Economia y Competitividad-Spain (MINECO) [CTQ2015-67870-P]
- Generalitat de Catalunya [2017 SGR 1439, GGC2017A-SGR-1488]
- Marato TV3 [201C/2018]
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Novel antibiotic compounds have been prepared through a selective multicomponent reaction upon the known drug Trimethoprim. The Groebke-Blackburn-Bienayme reaction involving this alpha-aminoazine, with a range of aldehydes and isocyanides afforded the desired adducts in one-step. The analogs display meaningful structural features of the initial drug together with relevant modifications at several points, keeping antibiotic potency and showing satisfactory antimicrobial profile (good activity levels and reduced growth rates), especially against methicillin-resistant Staphylococcus aureus. The new products may open new possibilities to fight bacterial infections.
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