874899-41-9

Upstream product

• 874899-40-8 N-{4-(hydroxymethyl)-5-[3-(methylthio)benzyl]-1,3-thiazol-2-yl}acetamide 
• 874899-38-4 ethyl 2-amino-5-[3-(methylthio)benzyl]-1,3-thiazole-4-carboxylate 
• 874899-37-3 ethyl 3-bromo-4-[3-(methylthio)phenyl]-2-oxobutanoate 
• 874899-36-2 ethyl 4-[3-(methylthio)phenyl]-2-oxobutanoate 
• 874899-35-1 methyl 3-[3-(methylthio)phenyl]propanoate 
• 874899-34-0 methyl (2E)-3-[3-(methylsulfanyl)phenyl]acrylate 
• 616196-32-8 N-methoxy-N-methyl-3-(methylsulfanyl)benzamide 
• 825-99-0 3-methylsulfanyl-benzoic acid 
• 73771-35-4 3-(methylsulfanyl)benzaldehyde 
• 874899-39-5 ethyl 2-(acetylamino)-5-[3-(methylthio)benzyl]-1,3-thiazole-4-carboxylate 

Downstream Products

• 874899-42-0 N-{5-[3-(methylthio)benzyl]-4-[(Z)-2-(4-nitrophenyl)vinyl]-1,3-thiazol-2-yl}acetamide 
• 737826-70-9 di-tert-butyl ({[4-(2-{2-(acetylamino)-5-[3-(methylsulfonyl)benzyl]-1,3-thiazol-4-yl}ethyl)phenyl]amino}methylidene)biscarbamate 
• 794459-66-8 N-{4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-5-[3-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}acetamide 

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: Part 2

Novel thiazole derivatives were synthesized and evaluated as vascular adhesion protein-1 (VAP-1) inhibitors. Although our previous compound 1 showed potent VAP-1 inhibitory activity, the activity differed between humans and rats. This issue was overcome by a hybrid design using human VAP-1 specific inhibitor 2, which was found by high-throughput screening (HTS), a docking study of a human VAP-1 homology model, and an analysis of sequence information for humans and rats. As a result, we identified compound 35c, which showed strong VAP-1 inhibitory activity (human IC50 of 20 nM; rat IC50 of 72 nM) and significant inhibitory effects in the ex vivo test.

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.