Bioorganic and Medicinal Chemistry Letters p. 5740 - 5743 (2013)
Update date:2022-08-05
Topics:
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.
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.
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