Yamaki, Susumu published the artcileSynthesis and pharmacological evaluation of glycine amide derivatives as novel vascular adhesion protein-1 inhibitors without CYP3A4 and CYP2C19 inhibition, HPLC of Formula: 887425-47-0, the main research area is glycine amide derivative preparation vascular adhesion protein VAP1 inhibitor; diabetic nephropathy treatment glycine amide derivative VAP1 inhibitor; CYP2C19; CYP3A4; Diabetic nephropathy; Glycine amide; Vascular adhesion protein-1.
Vascular adhesion protein-1 (VAP-1) is a promising therapeutic target for the treatment of diabetic nephropathy. Here, the authors conducted optimization studies of the authors’ lead compound 1 (I), which the authors previously reported as a novel VAP-1 inhibitor, to enhance the inhibition of human VAP-1 and to reduce CYP3A4 and CYP2C19 inhibition. As a result, the authors identified 3-chloro-4-{4-[5-(3-{[glycyl(methyl)amino]methyl}phenyl)pyrimidin-2-yl]piperazin-1-yl}benzoic acid (17h) as a novel orally active VAP-1 inhibitor, with 14-fold increased human VAP-1 inhibitory activity compared to 1, without CYP3A4 and CYP2C19 inhibition. Oral administration of 17h significantly inhibited the progression of proteinuria in streptozotocin (STZ) induced diabetic rats at 0.3 and 1 mg/kg, suggesting that this compound has potential to be a therapeutic agent for the treatment of diabetic nephropathy.
Bioorganic & Medicinal Chemistry published new progress about Bioactive lead compounds (optimization). 887425-47-0 belongs to class piperidines, name is 1-(5-Bromopyrimidin-2-yl)piperidin-4-ol, and the molecular formula is C9H12BrN3O, HPLC of Formula: 887425-47-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem