Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions.

Antibiotics (Basel)

Laboratory of Molecular Microbiology & Antimicrobials, Department of Pathology & Experimental Therapeutics, Medical School, University of Barcelona and IDIBELL, Feixa Llarga, s/n, 08907 Hospitalet de Llobregat, Spain.

Published: January 2023

New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against Mycolata bacteria. Microbiological guidance for medicinal chemistry is a powerful tool to design new and effective antimicrobials. In this case, the readily synthesized compounds open new possibilities in the search for antimicrobials active on mycolic acid-containing bacteria.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9854905PMC
http://dx.doi.org/10.3390/antibiotics12010083DOI Listing

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