Phthalylsulfacetamide

Phthalylsulfacetamide is an orally active sulfonamide antibiotic and New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC₅₀ of 15.4 μM. Phthalylsulfacetamide stably binds to the active hydrolysis center of NDM-1, interacts with Zn²⁺, and interacts with key amino acid residues Val73 and His122 to inhibit enzyme activity. Phthalylsulfacetamide can be used for the research of Escherichia coli infection^[1]. In Vitro:Phthalylsulfacetamide (4-128 μM) potently inhibits purified recombinant NDM-1 enzyme activity with an IC₅₀ of 15.4 μM^[1].
Phthalylsulfacetamide (16 h) alone exhibits negligible intrinsic antibacterial activity against NDM-1-positive Escherichia coli with an MIC of 512 μg/mL^[1].
Phthalylsulfacetamide (16 h) acts synergistically with Meropenem (HY-13678) against NDM-1-positive Escherichia coli, reducing Meropenem's MIC by 32-fold with an FICI of 0.156^[1].
Phthalylsulfacetamide (64 μg/mL), when combined with Meropenem, rapidly eliminates NDM-1-positive Escherichia coli within 3 h, with no regrowth observed^[1].
Phthalylsulfacetamide (1-8 mg/mL; 24 h) exhibits no significant cytotoxicity toward mouse small intestinal mucosal epithelial cells^[1]. In Vivo:Phthalylsulfacetamide (5-20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, dose-dependently reduces bacterial load, white blood cell counts, and proinflammatory cytokine levels in mice with systemic NDM-1-positive E. coli infection^[1].
Phthalylsulfacetamide (20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, increases survival rate to 70% in mice with lethal systemic NDM-1-positive E. coli infection^[1].
Phthalylsulfacetamide (20 mg/kg; i.g.; every 12 hours; 6 doses), when combined with Meropenem, reduces bacterial load, white blood cell counts, and proinflammatory cytokine levels, and alleviates histopathological damage in mice with sublethal systemic NDM-1-positive E. coli infection, while monotherapy only reduces small intestine bacterial load^[1].