77505-86-3

Upstream product

• 64920-29-2 2-oxo-4-phenylbutanoic acid ethyl ester 
• 17356-08-0 thiourea 
• 292858-05-0 ethyl 3-bromo-2-oxo-4-phenylbutanoate 

Downstream Products

• 874964-11-1 di-tert-butyl [(Z)-({4-[2-(2-(acetylamino)-5-{4-[(dimethylamino)sulfonyl]benzyl}-1,3-thiazol-4-yl)ethyl]phenyl}amino)methylidene]biscarbamate 
• 874964-09-7 di-tert-butyl ((Z)-{[4-(2-{2-(acetylamino)-5-[4-(aminosulfonyl)benzyl]-1,3-thiazol-4-yl}ethyl)phenyl]amino}methylidene)biscarbamate 
• 874899-63-5 N-(4-[2-(4-aminophenyl)ethyl]-5-{4-[(dimethylamino)sulfonyl]benzyl}-1,3-thiazol-2-yl)acetamide 
• 874899-61-3 N-{4-[2-(4-aminophenyl)ethyl]-5-[4-(aminosulfonyl)benzyl]-1,3-thiazol-2-yl}acetamide 
• 737824-45-2 di-tert-butyl {(Z)-[(4-{2-[2-(acetylamino)-5-benzyl-1,3-thiazol-4-yl]ethyl}phenyl)amino]methylidene}biscarbamate 
• 737824-44-1 N-{4-[2-(4-aminophenyl)ethyl]-5-benzyl-1,3-thiazol-2-yl}acetamide 
• 737824-43-0 N-{5-benzyl-4-[2-(4-nitrophenyl)vinyl]-1,3-thiazol-2-yl}acetamide 
• 737824-42-9 N-(5-benzyl-4-formyl-1,3-thiazol-2-yl)acetamide 
• 737824-41-8 ethyl 2-(acetylamino)-5-benzyl-1,3-thiazole-4-carboxylate 

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.

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