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

Trejo, Angela, Carme Masdeu, Irene Serrano-Pérez, Marina Pedrola, Narcís Juanola, Ouldouz Ghashghaei, Guadalupe Jiménez-Galisteo, Rodolfo Lavilla, Francisco Palacios, Concepción Alonso, and Viñas, Miquel.

https://doi.org/10.3390/antibiotics12010083

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.