Compound ID | 2871

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APL-2301

Synonym(s): MET-102  |  ASN-1733

Class: Membrane-active agent

Agent Type: Synthetic; Small molecule; Direct acting;
Spectrum of activity: Gram-positive & Gram-negative
Mechanism of action: Membrane-active agent. Disrupts integrity of cell membrane and inhibits NDM
Target Pathogen: Active against Staphylococcus aureus, Escherichia coli, and other NDM-producing strains
Description: Synthetic compound derived from nitroxoline (5-nitro-8-hydroxyquinoline) scaffold; shows synergistic effect with meropenem against NDM-1 producing strains; cytotoxic (IC50) and haemolytic activity only at concentrations >12xMIC50
Institute where first reported: Asieris Pharmaceuticals
Year first mentioned: 2024
Highest development stage: Phase 1 (to begin in Australia in 2024)
Development status: Active
Chemical structure(s):
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Molecular weight: 303.5
Iso. SMILES: C1=CC2=C(C(=C(C(=C2Cl)Br)[N+](=O)[O-])O)N=C1
InChI Key: BZGYNSYRIWILNU-UHFFFAOYSA-N
Can. SMILES: C1=CN=C2C(=C1)C(=C(C(=C2O)[N+](=O)[O-])Br)Cl
InChI: InChI=1S/C9H4BrClN2O3/c10-5-6(11)4-2-1-3-12-7(4)9(14)8(5)13(15)16/h1-3,14H
External links:
Guide to Pharmacology: APL-2301
Citation: https://www.tandfonline.com/doi/full/10.1080/22221751.2023.2294854

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