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

…, A Kulkarni-Almeida, D Bhedi, RA Vishwakarma

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5740 - 5743

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Citation Number: 5

Abstract

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- ...