Sulfamethizole exhibits multifaceted bioactivities across various biological pathways and targets. It displays significant antibacterial properties against Escherichia coli, Bacillus subtilis, and Klebsiella pneumoniae, with a dose-dependent increase in the zone of inhibition, highlighting its potency at higher concentrations. Specifically, it inhibits Escherichia coli Dihydropteroate synthase (EII50 = 0.4) and the growth of Escherichia coli (GII50 = 750.0). It also shows inhibition of Cytochrome P450 3A4 with an IC50 of 835,603.02 nM and has intrinsic solubility in water at 450.0 µg/mL.
Furthermore, Sulfamethizole demonstrates a range of inhibitory activities, including Lamin A splicing, ALDH1A1, Anthrax Lethal Toxin Internalization, AmpC Beta-Lactamase, HP1-beta Chromodomain Interactions, peroxisome proliferator-activated receptor delta signaling, DNA re-replication in normal breast cells, and USP1/UAF1. It also shows potential against Plasmodium falciparum with a potency of 1,882.1 nM and inhibiting viability of multiple cancer cell lines with an IC50 of 20,000.0 nM. Additionally, it exhibits antiviral activity against SARS-CoV-2, inhibiting virus-induced cytotoxicity in various assays, though with limited efficacy indicated by hit scores and percentages.
The compound has a high plasma protein binding of 93.5%, a log D distribution coefficient of -1.33 at pH 7.4, and a pKa value of 5.4. It has also demonstrated hepatotoxicity without severe liver conditions and is involved in Drug Induced Liver Injury (DILI) prediction datasets. Sulfamethizole significantly inhibits sodium fluorescein uptake in OATP1B1-transfected and OATP1B3-transfected CHO cells, and shows weak inhibitory activity against human BSEP.
Overall, Sulfamethizole exhibits extensive bioactivity with potential implications in antibacterial, antiviral, and enzymatic inhibition applications, while also showing some cytotoxic and hepatotoxic effects..
Note: Summary generated by AI. Data source: ChEMBL 