WRR-483, an analogue of K-11777, is a potent and selective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. WRR-483 demonstrates good potency against cruzain with sensitivity to pH conditions and high efficacy in the cell culture assay. Furthermore, WRR-483 also eradicates parasite infection in a mouse model of acute Chagas' disease. WRR-483 binds covalently to the active site cysteine of the protease in a similar manner as other vinyl sulfone-based inhibitors. WRR-483 has potential to be developed as a treatment for Chagas' disease.
Famotidine propionic acid is a histamine H2-receptor antagonist that inhibits stomach acid production. It is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease.
OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea