2. Academic Validation
  3. 1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties

1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties

  • J Med Chem. 2002 Jun 6;45(12):2362-5. doi: 10.1021/jm025522z.
Edwin B Villhauer,  John A Brinkman,  Goli B Naderi,  Beth E Dunning,  Bonnie L Mangold,  Manisha D Mone,  Mary E Russell,  Stephen C Weldon,  Thomas E Hughes
PMID: 12036346 DOI: 10.1021/jm025522z
Abstract

Dipeptidyl Peptidase IV (DPP-IV) inhibition has the potential to become a valuable therapy for type 2 diabetes. We report the first use of solid-phase synthesis in the discovery of a new DPP-IV inhibitor class and a solution-phase synthesis that is practical up to the multikilogram scale. One compound, NVP-DPP728 (2), is profiled as a potent, selective, and short-acting DPP-IV inhibitor that has excellent oral bioavailability and potent antihyperglycemic activity.

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