New diarylpentanoids and chalcones as potential antimicrobial adjuvants

• Type: Article in International Scientific Journal
• Date: 2022

Authors

Moreira J. (Author) Other; Durães F. (Author) Other; Freitas-Silva J. (Author) Other; Szemerédi N. (Author) Other; Resende D.I.S.P. (Author) Other; Eugenia Pinto (Author) FFUP; da Costa P.M. (Author) Other; Pinto M. (Author) Other; Spengler G. (Author) Other; Honorina Cidade (Author) FFUP; Emilia Sousa (Author) FFUP

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 67

ISSN: 0960-894X

Publisher: Elsevier

Indexing

Scopus - 4 Citations

Other information

Authenticus ID: P-00W-FRP

DOI: 10.1016/j.bmcl.2022.128743

Abstract (EN): Antimicrobial resistance arises due to several adaptation mechanisms, being the overexpression of efflux pumps (EPs) one of the most worrisome. In bacteria, EPs can also play important roles in virulence, quorum-sensing (QS) and biofilm formation. To identify new potential antimicrobial adjuvants, a library of diarylpentanoids and chalcones was synthesized and tested. These compounds presented encouraging results in potentiating the activity of antimicrobials, being diarylpentanoid 13 the most promising. Compounds 9, 13, 16, 19, 22, and 23 displayed EP inhibitory effect, mainly in Staphylococcus aureus 272123. Compounds 13, 19, 22, and 23 exhibited inhibitory effect on biofilm formation in S. aureus 272,123 while 13 and 22 inhibited QS in the pair Sphingomonas paucimobilis Ezf 10¿17 and Chromobacterium violaceum CV026. The overall results, demonstrated that diarylpentanoid 13 and chalcone 22 were active against all the resistance mechanisms tested, suggesting their potential as antimicrobial adjuvants.

Language: English

Type (Professor's evaluation): Scientific