737825-27-3

Upstream product

• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 737825-25-1 N-{5-(4-iodobenzyl)-4-[2-(4-nitrophenyl)vinyl]-1,3-thiazol-2-yl}acetamide 
• 737825-24-0 N-[4-formyl-5-(4-iodobenzyl)-1,3-thiazol-2-yl]acetamide 
• 737825-23-9 ethyl 2-(acetylamino)-5-(4-iodobenzyl)-1,3-thiazole-4-carboxylate 
• 737825-22-8 ethyl 2-amino-5-(4-iodobenzyl)-1,3-thiazole-4-carboxylate hydrobromide 
• 737825-21-7 ethyl 3-bromo-4-(4-iodophenyl)-2-oxobutanoate 
• 737825-20-6 ethyl 4-(4-iodophenyl)-2-oxobutanoate 
• 1443744-28-2 C₁₃H₁₃IN₂O₂S 
• 157126-75-5 4-iodobenzenepropanoic acid,ethyl ester 
• 2767-70-6 (p-nitrobenzyl)triphenylphosphonium bromide 
• 100-11-8 1-bromomethyl-4-nitro-benzene 

Downstream Products

• 737825-28-4 methyl 4-({2-(acetylamino)-4-[2-(4-aminophenyl)ethyl]-1,3-thiazol-5-yl}methyl)benzoate 
• 737825-29-5 methyl 4-[(2-(acetylamino)-4-{2-[4-({(Z)-[(tert-butoxycarbonyl)amino][(tert-butoxycarbonyl)imino]methyl}-amino)phenyl]ethyl}-1,3-thiazol-5-yl)methyl]benzoate 
• 737825-19-3 methyl 4-({2-(acetylamino)-4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-1,3-thiazol-5-yl}methyl)benzoate 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: 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.