874901-20-9

Basic information

• Product Name: N-[4-((E)-2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}vinyl)-1,3-thiazol-2-yl]acetamide
• Synonyms: N-[4-((E)-2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}vinyl)-1,3-thiazol-2-yl]acetamide
• CAS NO: 874901-20-9
• Molecular Weight: 417.488
• Mol File: 874901-20-9.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: N-[4-((E)-2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}vinyl)-1,3-thiazol-2-yl]acetamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-[4-((E)-2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}vinyl)-1,3-thiazol-2-yl]acetamide(874901-20-9)
• EPA Substance Registry System: N-[4-((E)-2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}vinyl)-1,3-thiazol-2-yl]acetamide(874901-20-9)

Safety Data

• Hazardous Substances Data: 874901-20-9(Hazardous Substances Data)

Upstream product

• 1074-82-4 potassium phtalimide 
• 7617-70-1 4-(2-Bromoethyl)benzaldehyde 
• 7460-59-5 N-(4-(chloromethyl)thiazol-2-yl)acetamide 
• 874901-18-5 4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]benzaldehyde 
• 874899-73-7 {[2-(acetylamino)-1,3-thiazol-4-yl]methyl}(triphenyl)phosphonium chloride 

Downstream Products

• 874901-22-1 N-[4-(2-{4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethyl]phenyl}ethyl)-1,3-thiazol-2-yl]acetamide 
• 776295-05-7 N-(4-{2-[4-(2-aminoethyl)phenyl]ethyl}-1,3-thiazol-2-yl)acetamide 

Relevant articles and documents

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 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.