874900-00-2

Upstream product

• 737824-50-9 ethyl 2-(acetylamino)-5-[4-(methylthio)benzyl]-1,3-thiazole-4-carboxylate 
• 63545-55-1 [3-(4-mercaptoethyl)]propanoic acid 
• 123392-44-9 methyl 3-[4-(methylthio)phenyl]propanoate 
• 737824-47-4 ethyl 4-[4-(methylthio)phenyl]-2-oxobutanoate 
• 737824-48-5 ethyl 3-bromo-4-[4-(methylthio)phenyl]-2-oxobutanoate 
• 737824-49-6 ethyl 2-amino-5-[4-(methylthio)benzyl]-1,3-thiazole-4-carboxylate 

Downstream Products

• 737824-53-2 N-{5-[4-(methylsulfonyl)benzyl]-4-[2-(4-nitrophenyl)vinyl]-1,3-thiazol-2-yl}acetamide 
• 737824-46-3 N-{4-[2-(4-aminophenyl)ethyl]-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}acetamide 
• 1429659-70-0 tert-butyl {(Z)-{[4-(2-{2-acetamido-5-[4-(methylsulfanyl)benzyl]-1,3-thiazol-4-yl}ethyl)phenyl]amino}-[(tert-butoxycarbonyl)amino]methylene}carbamate 
• 737824-55-4 di-tert-butyl ((Z)-{[4-(2-{2-(acetylamino)-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-4-yl}ethyl)phenyl]amino}-methylidene)biscarbamate 
• 737824-92-9 N-{4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-5-[4-(methylthio)benzyl]-1,3-thiazol-2-yl}acetamide 
• 737824-54-3 N-{4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}acetamide 
• 737824-52-1 N-{5-[4-(methylthio)benzyl]-4-[2-(4-nitrophenyl)vinyl]-1,3-thiazol-2-yl}acetamide 
• 737824-51-0 N-{4-formyl-5-[4-(methylthio)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.