183365-33-5

Upstream product

• 19975-56-5 2-methylsulfanyl-4,5-dihydrothiazoline 
• 183365-29-9 N-{4-(2-(4-aminophenyl)ethyl)-1,3-thiazol-2-yl}acetamide 
• 111608-67-4 [2-(acetylamino)-1,3-thiazol-4-yl]methyl acetate 
• 51307-38-1 N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]acetamide 
• 100-11-8 1-bromomethyl-4-nitro-benzene 
• 2767-70-6 (p-nitrobenzyl)triphenylphosphonium bromide 
• 16444-13-6 N-(4-formyl-1,3-thiazol-2-yl)acetamide 
• 737822-88-7 N-{4-[(Z)-2-(4-nitrophenyl)ethenyl]-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

Vascular adhesion protein-1 (VAP-1), an amine oxidase that is also known as a semicarbazide-sensitive amine oxidase (SSAO), is present in particularly high levels in human plasma, and is considered a potential therapeutic target for various inflammatory diseases, including diabetes complications such as macular edema. In our VAP-1 inhibitor program, structural modifications following high-throughput screening (HTS) of our compound library resulted in the discovery that thiazole derivative 10, which includes a guanidine group, shows potent human VAP-1 inhibitory activity (IC50 of 230 nM; rat IC 50 of 14 nM). Moreover, compound 10 exhibited significant inhibitory effects on ocular permeability in STZ-induced diabetic rats.

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