(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

@article{Kim20052R4oxo43trifluoromethyl56dihydro124tri,
  title={(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.},
  author={Dooseop Kim and Lei Wang and Maria G. Beconi and George J. Eiermann and Michael Hallsworth Greg Fisher and Huaibing He and Gerard J Hickey and Jennifer E Kowalchick and Barbara Leiting and Kathryn A Lyons and Frank Marsilio and Margaret E McCann and Reshma A Patel and Aleksandr V Petrov and Giovanna Scapin and Sangita B Patel and Ranabir Sinha Roy and Joseph S. K. Wu and Matthew J Wyvratt and Bei B. Zhang and Lan Zhu and Nancy A. Thornberry and Ann Weber},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 1},
  pages={141-51}
}
A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC(50) = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in… CONTINUE READING
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