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Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors

Kowalchick, Jennifer E ; Leiting, Barbara ; Pryor, Kellyann D ; Marsilio, Frank ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Eiermann, George J ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Reshma A ; Thornberry, Nancy A ; Weber, Ann E ; Kim, Dooseop

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5934-5939 [Peer Reviewed Journal]

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Title:
Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Author: Kowalchick, Jennifer E ; Leiting, Barbara ; Pryor, Kellyann D ; Marsilio, Frank ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Eiermann, George J ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Reshma A ; Thornberry, Nancy A ; Weber, Ann E ; Kim, Dooseop
Description: Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as dipeptidyl peptidase IV (DPP-4) inhibitors. The in vitro profile of these compounds is described, and in vivo efficacy and pharmacokinetics are also presented. Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5934-5939
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2007.07.100
Subjects: Dipeptidyl Peptidase IV ; Dpp-4 ; Dipeptidyl Peptidase IV Inhibitors ; Dpp-4 Inhibitors ; Β-Amino Amides ; Triazolopiperazine ; Triazolopiperazine-Based Β-Amino Amides ; Type 2 Diabetes ; Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors

Kowalchick, Jennifer E ; Leiting, Barbara ; Pryor, Kellyann D ; Marsilio, Frank ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Eiermann, George J ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Reshma A ; Thornberry, Nancy A ; Weber, Ann E ; Kim, Dooseop

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