Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
Angela Trejo,
Carme Masdeu,
Irene Serrano-Pérez,
Marina Pedrola,
Narcís Juanola,
Ouldouz Ghashghaei,
Guadalupe Jiménez-Galisteo,
Rodolfo Lavilla,
Francisco Palacios,
Concepción Alonso,
Miguel Viñas
Affiliations
Angela Trejo
Departamento de Química Orgánica I, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko, Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain
Carme Masdeu
Departamento de Química Orgánica I, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko, Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain
Irene Serrano-Pérez
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
Marina Pedrola
Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences and Institute of Biomedicine (IBUB), University of Barcelona, Av. de Joan XXIII, 27-31, 08028 Barcelona, Spain
Narcís Juanola
Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences and Institute of Biomedicine (IBUB), University of Barcelona, Av. de Joan XXIII, 27-31, 08028 Barcelona, Spain
Ouldouz Ghashghaei
Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences and Institute of Biomedicine (IBUB), University of Barcelona, Av. de Joan XXIII, 27-31, 08028 Barcelona, Spain
Guadalupe Jiménez-Galisteo
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
Rodolfo Lavilla
Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences and Institute of Biomedicine (IBUB), University of Barcelona, Av. de Joan XXIII, 27-31, 08028 Barcelona, Spain
Francisco Palacios
Departamento de Química Orgánica I, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko, Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain
Concepción Alonso
Departamento de Química Orgánica I, Facultad de Farmacia, Universidad del País Vasco/Euskal Herriko, Unibertsitatea (UPV/EHU), Paseo de la Universidad 7, 01006 Vitoria-Gasteiz, Spain
Miguel Viñas
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
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.
