848833-24-9Relevant academic research and scientific papers
Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening
Agrawal, Madhavi,Kharkar, Prashant,Moghe, Sonali,Mahajan, Tushar,Deka, Vaishali,Thakkar, Chandni,Nair, Amrutha,Mehta, Chirag,Bose, Julie,Kulkarni-Almeida, Asha,Bhedi, Dilip,Vishwakarma, Ram A.
supporting information, p. 5740 - 5743 (2013/10/01)
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.
