Synthesis and Antibacterial Activity of Polyalthic Acid Analogs

• Main Authors: Marcela Nunes Argentin (Author), Felipe de Paula Nogueira Cruz (Author), Ariana Borges Souza (Author), Elisa Marcela de Oliveira D'Aurea (Author), Jairo Kenupp Bastos (Author), Sérgio Ricardo Ambrósio (Author), Rodrigo Cassio Sola Veneziani (Author), Ilana Lopes Baratella Cunha Camargo (Author), Cassia Suemi Mizuno (Author)
• Format: Book
• Published: MDPI AG, 2023-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

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 <i>Staphylococcus epidermidis</i> and determined the minimal inhibitory concentration (MIC) of the best analogs against planktonic bacterial cells. There was no difference in activity between the amides <b>2a</b> and <b>2b</b> and their corresponding amines <b>3a</b> and <b>3b</b> regarding their ability to eradicate biofilm. PA analogs <b>2a</b> and <b>3a</b> were able to significantly eradicate the preformed biofilm of <i>S. epidermidis</i> and were active against all the Gram-positive bacteria tested (<i>Enterococcus faecalis</i>, <i>Enterococcus faecium</i>, <i>S. epidermidis</i>, <i>Staphylococcus aureus)</i>, with different MIC depending on the microorganism. Therefore, PA analogs <b>2a</b> and <b>3a</b> are of interest for further in vitro and in vivo testing to develop formulations for antibiotic drugs against Gram-positive bacteria.

Item Description

10.3390/antibiotics12071202
2079-6382