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Multicomponent Reactions Upon the Known Drug Trimethoprim as a Source of Novel Antimicrobial Agents.

ABSTRACT: Novel antibiotic compounds have been prepared through a selective multicomponent reaction upon the known drug Trimethoprim. The Groebke-Blackburn-Bienaymé reaction involving this ?-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.

SUBMITTER: Pedrola M

PROVIDER: S-EPMC6621506 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Multicomponent Reactions Upon the Known Drug Trimethoprim as a Source of Novel Antimicrobial Agents.

Pedrola Marina M Jorba Marta M Jardas Eda E Jardi Ferran F Ghashghaei Ouldouz O Viñas Miguel M Lavilla Rodolfo R

Frontiers in chemistry 20190704

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 ...[more]

PMID: 31334221

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