| Identification | Back Directory | [Name]
1-(Pyridin-4-ylmethyl)-1H-imidazole-2-carboxylic acid | [CAS]
1439899-44-1 | [Synonyms]
Metallo-β-lactamase-IN-6
1-(Pyridin-4-ylmethyl)-1H-imidazole-2-carboxylic acid
1H-Imidazole-2-carboxylic acid, 1-(4-pyridinylmethyl)- | [Molecular Formula]
C10H9N3O2 | [MDL Number]
MFCD26097038 | [MOL File]
1439899-44-1.mol | [Molecular Weight]
203.2 |
| Hazard Information | Back Directory | [Uses]
Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL[1]. | [in vivo]
Metallo-β-lactamase-IN-6 (100 mg/kg; IP; single) reaches plasma concentration peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 is 1.24 hours[1].
Metallo-β-lactamase-IN-6 (500, 1000, or 2000 mg/kg; IP; single, observe for 14 days) does not result in any significant toxic effects and is well-tolerated by mice at a dose of ≤ 2000 mg/kg[1].
Pharmacokinetic Parameters of Metallo-β-lactamase-IN-6 in male female ICR mice[1].
| IP (100 mg/kg) | | T1/2 (h) | 1.243 | | Cmax (μg/mL) | 142.8 | | Tmax (h) | 0.151 | | Vd (mL/kg) | 535.804 | | CL (mL/h/kg) | 248.512 | | AUC0-∞ (μg/mL·h) | 896 |
| Animal Model: | Female ICR mice (180-220 g)[1] | | Dosage: | 100 mg/kg | | Administration: | IP; single (Pharmacokinetics Analysis) | | Result: | Plasma concentration reached its peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 was 1.24 hours. |
| Animal Model: | Female ICR mice (n=5)[1] | | Dosage: | 500, 1000, or 2000 mg/kg | | Administration: | IP; single, observed for 14 days | | Result: | Did not result in any significant toxic effects and was well-tolerated by mice at a dose of ≤ 2000 mg/kg. |
| [References]
[1] Yan YH, Li W, Chen W, et al. Structure-guided optimization of 1H-imidazole-2-carboxylic acid derivatives affording potent VIM-Type metallo-β-lactamase inhibitors. Eur J Med Chem. 2022;228:113965. DOI:10.1016/j.ejmech.2021.113965 |
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