737824-45-2

Upstream product

• 77505-86-3 ethyl 2-amino-5-benzyl-1,3-thiazole-4-carboxylate 
• 292858-05-0 ethyl 3-bromo-2-oxo-4-phenylbutanoate 
• 2767-70-6 (p-nitrobenzyl)triphenylphosphonium bromide 
• 100-11-8 1-bromomethyl-4-nitro-benzene 
• 64920-29-2 2-oxo-4-phenylbutanoic acid ethyl ester 
• 737824-44-1 N-{4-[2-(4-aminophenyl)ethyl]-5-benzyl-1,3-thiazol-2-yl}acetamide 
• 152120-54-2 N,N'-bis( tert-butoxycarbonyl)-1H-pyrazole-1-carboxamidine 
• 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 

Downstream Products

• 737824-40-7 N-{4-[2-(4-{[amino(imino)methyl]amino}phenyl)ethyl]-5-benzyl-1,3-thiazol-2-yl}acetamide 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.

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