Li, Rong published the artcileDesign, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors, Product Details of C9H8N2O2, the main research area is imidazole carboxylic acid derivative metallo beta lactamase inhibitor; Antibiotic resistance; Metal-binding pharmacophore; Metallo-β-lactamase; Structure-activity relationship; VIM.
As one of important mechanisms to beta-lactam antimicrobial resistance, metallo-β-lactamases (MBLs) have been receiving increasing worldwide attentions. Ambler subclass B1 MBLs are most clin. relevant, because they can hydrolyze almost all beta-lactams with the exception of monobactams. However, it is still lacking of clin. useful drugs to combat MBL-medicated resistance. We previously identified 1H-imidazole-2-carboxylic acid as a core metal-binding pharmacophore (MBP) to target multiple B1 MBLs. Herein, we report structural optimization of 1H-imidazole-2-carboxylic acid and substituents. Structure-activity relationship (SAR) analyses revealed that replacement of 1H-imidazole-2-carboxylic acid with other structurally highly similar MBPs excepting thiazole-4-carboxylic acid resulted in decreased MBL inhibition. Further SAR studies identified more potent inhibitors to MBLs, of which 28 manifested IC50 values of 0.018 μM for both VIM-2 and VIM-5. The microbiol. tests demonstrated that the most tested compounds showed improved synergistic effects; some compounds at 1 μg/mL were able to reduce meropenem MIC by at least 16-fold, which will be worth further development of new potent inhibitors particularly targeting VIM-type MBLs.
Bioorganic & Medicinal Chemistry published new progress about Antimicrobial agent resistance. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Product Details of C9H8N2O2.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem