Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587663 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Madhavi Agrawal, Prashant Kharkar, Sonali Moghe, Tushar Mahajan, Vaishali Deka, Chandni Thakkar, Amrutha Nair, Chirag Mehta, Julie Bose, Asha Kulkarni-Almeida, Dilip Bhedi, Ram A. Vishwakarma,