1302012-28-7

Upstream product

• 85-44-9 phthalic anhydride 
• 57691-07-3 ethyl [(E)-3-oxo-1,3-dihydroisobenzofuran-1-ylidene]acetate 
• 25947-13-1 ethyl 1,2-dihydro-1-oxophthalazin-4-ylacetate 
• 356790-62-0 ethyl 2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetate 
• 65705-44-4 2-amino-4-(4’-bromophenyl)-5-methyl-1,3-thiazole 
• 28081-52-9 2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid 

Relevant academic research and scientific papers

Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening

With the aim to discover orally active small molecules that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl- phthalazinone acetamide (7114863) increased glucose uptake (EC50 of 0.07 ± 0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, 7114863 was superior to rosiglitazone under similar experimental conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.