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

@article{Agrawal2013DiscoveryOT,
  title={Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.},
  author={Madhavi Agrawal and Prashant S. Kharkar and Sonali Moghe and Tushar R Mahajan and Vaishali Deka and Chandni S Thakkar and Amrutha V. Nair and Chirag B Mehta and Julie S. Bose and Asha A Kulkarni-Almeida and Dilip Bhedi and Ram A Vishwakarma},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 20},
  pages={5740-3}
}
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… CONTINUE READING