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Title: Multicomponent Reactions upon the Known Drug Trimethoprim as a Source of Novel Antimicrobial Agents
Author: Pedrola, Marina
Jorba, Marta
Jardas, Eda
Jardi, Ferran
Ghashghaei, Ouldouz
Viñas, Miquel
Lavilla Grífols, Rodolfo
Keywords: Antibiòtics
Issue Date: 4-Jul-2019
Publisher: Frontiers Media
Abstract: Novel antibiotic compounds have been prepared through a selective multicomponent reaction upon the known drug Trimethoprim. The Groebke-Blackburn-Bienaymé reaction involving this α-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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It is part of: Frontiers in Chemistry, 2019, vol. 7, p. 475
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ISSN: 2296-2646
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)

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