Discovery of 6-(aminomethyl)-5-(2, 4-dichlorophenyl)-7-methylimidazo [1, 2-a] pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors

…, J Marcinkeviciene, SP O'Connor…

Index: Meng, Wei; Brigance, Robert P.; Chao, Hannguang J.; Fura, Aberra; Harrity, Thomas; Marcinkeviciene, Jovita; O'connor, Stephen P.; Tamura, James K.; Xie, Dianlin; Zhang, Yaqun; Klei, Herbert E.; Kish, Kevin; Weigelt, Carolyn A.; Turdi, Huji; Wang, Aiying; Zahler, Robert; Kirby, Mark S.; Hamann, Lawrence G. Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5620 - 5628

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Citation Number: 25

Abstract

Continued structure− activity relationship (SAR) exploration within our previously disclosed azolopyrimidine containing dipeptidyl peptidase-4 (DPP4) inhibitors led us to focus on an imidazolopyrimidine series in particular. Further study revealed that by replacing the aryl substitution on the imidazole ring with a more polar carboxylic ester or amide, these compounds displayed not only increased DPP4 binding activity but also significantly ...