Pentamidine - Europe PMC

Repurposing Non-Antibiotic Drugs Auranofin and Pentamidine in Combination to Combat Multidrug-Resistant Gram-Negative Bacteria.

"Three days, the shortage of effective antibiotics against MDR Gram-negative bacterial infections, including auranofin and pentamidine, are being repurposed to treat MDR Gram-negative bacteria using a mixed strategy. Methods Chequerboard microdilution assay was used to determine the interaction of auranofin and pentamidine against drug-susceptible and MDR Gram-negative bacteria. With the combination therapy, bacterial membrane disruption caused by pentamidine treatment at sub-MIC resulted in an elevated intracellular auranofin concentration. The auranofin resistance growth in clinically isolated MDR bacteria was slower than the combination of auranofin and colistin, which is a last-line antibiotic with a membrane-lytic antibacterial function, according to the MDR bacteria. Conclusions The combination of non-antibiotic drugs with complementing antibacterial functions provides a potentially useful way to find new antibacterial drugs and delay drug resistance development. ".

Source link: https://europepmc.org/article/MED/35378227

Preclinical Development of Pentamidine Analogs Identifies a Potent and Nontoxic Antibiotic Adjuvant.

"While many new perturbants have been found in recent years, the majority of these molecules are unlikely to toxicity due to similarities between pathogen and host cell membrane membranes. We took a medicinal chemistry approach to produce pentamidine analogs with the aim of raising its OM activity while still minimizing its off-target toxicity. In Acinetobacter baumannii and Klebsiella pneumoniae, we discovered P35, which causes OM disruption and potentiates Gram-positive-active antibiotics. P35 has reduced mammalian cell cytotoxicity and hERG trafficking inhibition relative to pentamidine. In addition, P35 outperforms pentamidine in a murine model of A. baumannii bacteremia. ".

Source link: https://europepmc.org/article/MED/35319198

Pentamidine Ninety Years on: the Development and Applications of Pentamidine and its Analogs.

"This mini review examines pentamidine and its derivatives' development and use in the hopes of providing more pentamidine derivatives in the coming decades. ".

Source link: https://europepmc.org/article/MED/35289252

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