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Beschreibung

An orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial beta-glucuronidase activity (IC50 = 283 nM, kcat/Km = 0.0987 s-1µ,M-1, Ki = 164 nM in vitro assays against E coli beta-glucuronidase, EC50 = 17.7 nM in beta-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian beta-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli beta-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>>100 µ,M for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µ,g, p.o., b.i.d).