Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

RP Brigance, W Meng, A Fura, T Harrity, A Wang…

Index: Brigance, Robert P.; Meng, Wei; Fura, Aberra; Harrity, Thomas; Wang, Aiying; Zahler, Robert; Kirby, Mark S.; Hamann, Lawrence G. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 15 p. 4395 - 4398

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Citation Number: 33

Abstract

Several pyrazolo-, triazolo-, and imidazolopyrimidines were synthesized and evaluated as inhibitors of DPP4. Of these three classes of compounds, the imidazolopyrimidines displayed the greatest potency and demonstrated excellent selectivity over the other dipeptidyl peptidases. SAR evaluation for these scaffolds was described as they may represent potential treatments for type 2 diabetes.