Drug intelligence / Profile preview

Au(III)(C^S)-cyclometallated complex 1

Development stage
Preclinical
Lead developer
Barcelona Institute for Global Health
Modality
Small Molecules
01

Overview

Au(III)(C^S)-cyclometallated complex 1 is a novel cationic (C^S)-cyclometallated gold(III) dithiocarbamate complex being developed as an antibacterial and antibiofilm agent. It was co-developed by the University of Oviedo and the Barcelona Institute for Global Health (ISGlobal). The complex is synthesized via ligand substitution of the precursor [Au(dppta)Cl2] (where dppta is N,N-diisopropyl-P,P-diphenylphosphinothioic amide-κ2C,S) with 4-(hydroxymethyl)piperidine-1-carbodithioate, followed by precipitation with potassium hexafluorophosphate (KPF6). Au(III)(C^S)-cyclometallated complex 1 exhibits potent antibacterial and antibiofilm activity against multidrug-resistant (MDR) Gram-positive pathogens (such as Staphylococcus spp.) and Gram-negative pathogens. Its mechanism of action involves the disruption of bacterial membranes, induction of oxidative stress, and potent reversible inhibition of bacterial thioredoxin reductase.

Other names
[Au(dppta)(4-(hydroxymethyl)piperidine-1-carbodithioate)]+[Au(dppta)(4-(hydroxymethyl)piperidine-1-carbodithioate)]PF6Au(III) (C^S)-cyclometalated complex 1Au(III) (C^S)-cyclometallated complex 1Au(III)(C^S)-cyclometalated complex 1
02

Targets

TXNRD2 (Thioredoxin reductase 2)

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