Sulfisoxazole exhibits multifaceted bioactivity and pharmacokinetic properties, making it a significant compound for research. It shows potent inhibition of the Endothelin A receptor with an IC50 ranging from 780.0 nM to 9000.0 nM, indicating its strong interaction with this receptor in various systems, including rat aortic smooth muscle cells and human cells. Its binding affinity is much lower for the Endothelin B receptor, with an IC50 of 24000.0 nM.
Pharmacokinetically, Sulfisoxazole has high oral bioavailability (>80%) and significant plasma protein binding in humans (91.28%), dogs (86.59%), and rats (98.47%). It demonstrates moderate clearance rates and distribution, with a total clearance of 0.3 mL.min-1.kg-1 and a volume of distribution at steady state of 0.17 L.kg-1. Its physicochemical properties include a logD6.5 value of -0.5 and a pKa of 5.0.
Additionally, Sulfisoxazole exhibits bioactivity as an inhibitor of the Menin-MLL interaction, Thyroid Stimulating Hormone Receptor, Cytochrome P450 2C19, and various other targets. It shows antimicrobial activity against bacteria like Escherichia coli and Staphylococcus epidermidis, and antifungal activity against Aspergillus fumigatus, with MIC values indicating broad-spectrum bioactivity. Despite some liver toxicity and moderate liver clearance rates, it demonstrates low intrinsic clearance rates in rat hepatocytes and human liver microsomes, suggesting slow metabolism.
Sulfisoxazole also shows antiviral activity against SARS-CoV-2, albeit with limited effectiveness according to various assays, including cytotoxicity and 3CL-Pro protease inhibition. Furthermore, it has been identified to inhibit the Bile Salt Export Pump (BSEP), though at high IC50 values (>135000.0 nM), indicating weak inhibition.
Overall, Sulfisoxazole’s broad bioactivity profile, significant pharmacokinetic properties, and multi-target inhibition suggest its potential application in various therapeutic areas, albeit with caution due to its hepatotoxicity and moderate liver toxicity..
Note: Summary generated by AI. Data source: ChEMBL 