Exploration of Rhenium Bisquinoline Tricarbonyl Complexes for their Antibacterial Properties

TY - JOUR

T1 - Exploration of Rhenium Bisquinoline Tricarbonyl Complexes for their Antibacterial Properties

AU - Fulgencio, Sofia

AU - Scaccaglia, Mirco

AU - Frei, Angelo

N1 - Publisher Copyright: © 2024 The Authors. ChemBioChem published by Wiley-VCH GmbH.

PY - 2024/9/2

Y1 - 2024/9/2

N2 - Metal complexes have emerged as a promising source for novel classes of antibacterial agents to combat the rise of antimicrobial resistance around the world. In the exploration of the transition metal chemical space for novel metalloantibiotics, the rhenium tricarbonyl moiety has been identified as a promising scaffold. Here we have prepared eight novel rhenium bisquinoline tricarbonyl complexes and explored their antibacterial properties. Significant activity against both Gram-positive and Gram-negative bacteria was observed. However, all complexes also showed significant toxicity against human cells, putting into question the prospects of this specific rhenium compound class as metalloantibiotics. To better understand their biological effects, we conduct the first mode of action studies on rhenium bisquinoline complexes and show that they are able to form pores through bacterial membranes. Their straight-forward synthesis and tuneability suggests that further optimisation of this compound class could lead to compounds with enhanced bacterial specificity.

AB - Metal complexes have emerged as a promising source for novel classes of antibacterial agents to combat the rise of antimicrobial resistance around the world. In the exploration of the transition metal chemical space for novel metalloantibiotics, the rhenium tricarbonyl moiety has been identified as a promising scaffold. Here we have prepared eight novel rhenium bisquinoline tricarbonyl complexes and explored their antibacterial properties. Significant activity against both Gram-positive and Gram-negative bacteria was observed. However, all complexes also showed significant toxicity against human cells, putting into question the prospects of this specific rhenium compound class as metalloantibiotics. To better understand their biological effects, we conduct the first mode of action studies on rhenium bisquinoline complexes and show that they are able to form pores through bacterial membranes. Their straight-forward synthesis and tuneability suggests that further optimisation of this compound class could lead to compounds with enhanced bacterial specificity.

UR - http://www.scopus.com/inward/record.url?scp=85198526134&partnerID=8YFLogxK

U2 - 10.1002/cbic.202400435

DO - 10.1002/cbic.202400435

M3 - Article

C2 - 38785033

AN - SCOPUS:85198526134

SN - 1439-4227

VL - 25

JO - Chembiochem

JF - Chembiochem

IS - 17

M1 - e202400435

ER -