737823-72-2

Upstream product

• 737823-71-1 methyl 2-amino-5-[4-(methylthio)phenyl]-1,3-thiazole-4-carboxylate 
• 75-36-5 acetyl chloride 
• 1429659-56-2 methyl 3-bromo-3-[4-(methylsulfanyl)phenyl]-2-oxopropanoate 
• 737823-70-0 methyl 3-(4-(methylsulfanyl)phenyl)-2-oxopropanoate 
• 737823-69-7 3-(4-(methylsulfanyl)phenyl)-2-oxopropanoic acid 
• 3446-89-7 4-(Methylthio)benzaldehyde 

Downstream Products

• 737823-67-5 N-{4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-5-[4-(methylsulfonyl)phenyl]-1,3-thiazol-2-yl}acetamide hydrochloride 
• 737823-77-7 di-tert-butyl {[(4-{2-[2-(acetylamino)-5-(4-(methylsulfonyl)phenyl)-1,3-thiazol-4-yl]ethyl}phenyl)amino]-methylidene}biscarbamate 
• 737823-76-6 N-{4-[2-(4-aminophenyl)ethyl]-5-[4-(methylsulfonyl)phenyl]-1,3-thiazol-2-yl}acetamide 
• 737823-73-3 N-{4-formyl-5-[4-(methylsulfanyl)phenyl]-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 AND THEIR USE AS VAP-1 INHIBITORS

A compound of the formula (I): R1-NH-X-Y-Z (I) wherein R1 is acyl; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond, lower alkylene or -COHN-; and Z is a groupe of the formulae (II) or (III) wherein R