Sulfisoxazole

Sulfisoxazole is a sulfonamide antibiotic and nonpeptide endothelin (ET) receptor antagonist (IC₅₀s = 0.6 and 22 μM for the ET_A and ET_B receptors, respectively).^1,2 It inhibits the growth of Gram-positive and Gram-negative bacteria in vitro, including S. pneumoniae, B. subtilis, S. epidermidis, E. coli, and K. pneumoniae (MICs = 1.95, 0.98, 7.81, 62.5, and 7.81 μg/mL, respectively).³ Sulfisoxazole inhibits phosphoinositide turnover stimulated by endothelin-1 (ET-1; Item No. 24127) in TE671 cells. It inhibits ET-induced contraction of rat pulmonary artery rings ex vivo when used at concentrations of 0.1 and 1 mM.² Sulfisoxazole (1,000 mg/kg per day) reduces atrial natriuretic peptide levels in myocytes and plasma and increases survival in a rat model of pulmonary hypertension induced by monocrotaline (MCT; Item No. 16666) as well as blocks MCT-induced increases in pulmonary artery blood pressure when administered at doses of 300 and 1,000 mg/kg.

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1. Chan, M.F., Okun, I., Stavros, F.L., et al. Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening. Biochem. Bioph. Res. Commun. 201(1), 228-234 (1994).

2. Uchino, T., Sanyal, S.N., Yamabe, M., et al. Rescue of pulmonary hypertension with an oral sulfonamide antibiotic sulfisoxazole by endothelin receptor antagonistic actions. Hypertens. Res. 31(9), 1781-1790 (2008).

3. Nasr, T., Bondock, S., and Eid, S. Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety. Eur. J. Med. Chem. 84, 491-504 (2014).