The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
(2 R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8 H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Open accessAbstract
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 preclinical species, and in vivo efficacy in animal models. MK-0431, the phosphate salt of compound 1, was selected for development as a potential new treatment for type 2 diabetes.
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Kieffer, T. J., McIntosh, C. H., & Pederson, R. A. (1995) · Endocrinology · doi:10.1210/endo.136.8.7628397 · Cited by 1,124
Truncated GLP-1 (proglucagon 78?107-amide) inhibits gastric and pancreatic functions in man
Wettergren, A., Schjoldager, B., Mortensen, P. E., Myhre, J., Christiansen, J., & Holst, J. J. (1993) · Digestive Diseases and Sciences · doi:10.1007/bf01316798 · Cited by 670
Flint, A., Raben, A., Ersbøll, A., Holst, J., & Astrup, A. (2001) · International Journal of Obesity · doi:10.1038/sj.ijo.0801627 · Cited by 384
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The Many Roles for Fluorine in Medicinal Chemistry
Hagmann, W. K. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800219f · Cited by 3,578
The role of incretins in glucose homeostasis and diabetes treatment
Kim, W., & Egan, J. M. (2008) · Pharmacological Reviews · doi:10.1124/pr.108.000604 · Cited by 824
Charbonnel, B., Karasik, A., Liu, J., Wu, M., Meininger, G., & for the Sitagliptin Study 020 Group (2006) · Diabetes Care · doi:10.2337/dc06-0706 · Cited by 790
Raz, I., Hanefeld, M., Xu, L., Caria, C., Williams-Herman, D., Khatami, H., & Sitagliptin Study 023 Group (2006) · Diabetologia · doi:10.1007/s00125-006-0416-z · Cited by 614
Rosenstock, J., Brazg, R., Andryuk, P. J., Lu, K., & Stein, P. (2006) · Clinical Therapeutics · doi:10.1016/j.clinthera.2006.10.007 · Cited by 514
Metadata
- Authors
- Kim, D., Wang, L., Beconi, M., Eiermann, G. J., Fisher, M. H., He, H., Hickey, G. J., Kowalchick, J. E., Leiting, B., Lyons, K., Marsilio, F., McCann, M. E., Patel, R. A., Petrov, A., Scapin, G., Patel, S. B., Roy, R. S., Wu, J. K., Wyvratt, M. J., Zhang, B. B., Zhu, L., Thornberry, N. A., & Weber, A. E.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2004-12-13
- Volume
- 48
- Issue
- 1
- Pages
- 141-151
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2083473802
- Cited by
- 822
- References
- 4
- FWCI
- 24.61
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: (2 R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8 H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes. https://app.cochat.ai/papers/10.1021/jm0493156
- The paper
- Kim, D., Wang, L., Beconi, M., Eiermann, G. J., Fisher, M. H., He, H., Hickey, G. J., Kowalchick, J. E., Leiting, B., Lyons, K., Marsilio, F., McCann, M. E., Patel, R. A., Petrov, A., Scapin, G., Patel, S. B., Roy, R. S., Wu, J. K., Wyvratt, M. J., . . . Weber, A. E. (2005). (2 R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8 H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm0493156
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
