Synthesis and Antibacterial Activity of Polyalthic Acid Analogs
Marcela Nunes Argentin,
Felipe de Paula Nogueira Cruz,
Ariana Borges Souza,
Elisa Marcela de Oliveira D’Aurea,
Jairo Kenupp Bastos,
Sérgio Ricardo Ambrósio,
Rodrigo Cassio Sola Veneziani,
Ilana Lopes Baratella Cunha Camargo,
Cassia Suemi Mizuno
Affiliations
Marcela Nunes Argentin
Laboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, Brazil
Felipe de Paula Nogueira Cruz
Laboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, Brazil
Ariana Borges Souza
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, Brazil
Elisa Marcela de Oliveira D’Aurea
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, Brazil
Jairo Kenupp Bastos
School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café S/N, Ribeirão Preto 14040-930, SP, Brazil
Sérgio Ricardo Ambrósio
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, Brazil
Rodrigo Cassio Sola Veneziani
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, Franca 14404-600, SP, Brazil
Ilana Lopes Baratella Cunha Camargo
Laboratory of Molecular Epidemiology and Microbiology, Department of Physics and Interdisciplinary Science, São Carlos Institute of Physics, University of São Paulo, São Carlos 13563-120, SP, Brazil
Cassia Suemi Mizuno
College of Pharmacy and Health Sciences, Western New England University, Springfield, MA 01109, USA
Polyalthic acid (PA) is a diterpene found in copaiba oil. As a continuation of our work with PA, we synthesized PA analogs and investigated their antibacterial effects on preformed biofilms of Staphylococcus epidermidis and determined the minimal inhibitory concentration (MIC) of the best analogs against planktonic bacterial cells. There was no difference in activity between the amides 2a and 2b and their corresponding amines 3a and 3b regarding their ability to eradicate biofilm. PA analogs 2a and 3a were able to significantly eradicate the preformed biofilm of S. epidermidis and were active against all the Gram-positive bacteria tested (Enterococcus faecalis, Enterococcus faecium, S. epidermidis, Staphylococcus aureus), with different MIC depending on the microorganism. Therefore, PA analogs 2a and 3a are of interest for further in vitro and in vivo testing to develop formulations for antibiotic drugs against Gram-positive bacteria.
