874964-40-6

Upstream product

• 103454-18-8 5-(4-nitrophenyl)pentan-2-one 
• 874900-79-5 N-{4-[3-(4-aminophenyl)propyl]-1,3-thiazol-2-yl}acetamide 
• 152120-54-2 N,N'-bis( tert-butoxycarbonyl)-1H-pyrazole-1-carboxamidine 
• 183365-27-7 N-{4-[3-(4-nitrophenyl)propyl]-1,3-thiazol-2-yl}acetamide 
• 1426055-76-6 4-[3-(4-nitrophenyl)propyl]-1,3-thiazol-2-amine 

Downstream Products

• 874900-77-3 N-{4-[3-(4-{[amino(imino)methyl]amino}phenyl)propyl]-1,3-thiazol-2-yl}acetamide hydrochloride 

Relevant academic research and scientific papers

Synthesis and SAR study of new thiazole derivatives as vascular adhesion protein-1 (VAP-1) inhibitors for the treatment of diabetic macular edema

Vascular adhesion protein-1 (VAP-1), an amine oxidase that is also known as a semicarbazide-sensitive amine oxidase (SSAO), is present in particularly high levels in human plasma, and is considered a potential therapeutic target for various inflammatory diseases, including diabetes complications such as macular edema. In our VAP-1 inhibitor program, structural modifications following high-throughput screening (HTS) of our compound library resulted in the discovery that thiazole derivative 10, which includes a guanidine group, shows potent human VAP-1 inhibitory activity (IC50 of 230 nM; rat IC 50 of 14 nM). Moreover, compound 10 exhibited significant inhibitory effects on ocular permeability in STZ-induced diabetic rats.

THIAZOLE DERIVATIVES HAVING VAP-1 INHIBITORY ACTIVITY

A compound of the formula (I), (II), (III) or (IV): wherein each symbol is as defined in the specification,or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.