The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: A Potent, Selective, and Orally Bioavailable Dipeptidyl Peptidase IV Inhibitor with Antihyperglycemic Properties
Open accessAbstract
Dipeptidyl peptidase IV (DPP-IV) inhibition has the potential to become a valuable therapy for type 2 diabetes. The synthesis and structure-activity relationship of a new DPP-IV inhibitor class, N-substituted-glycyl-2-cyanopyrrolidines, are described as well as the path that led from clinical development compound 1-[2-[5-cyanopyridin-2-yl)amino]ethylamino]acetyl-2-cyano-(S)-pyrrolidine (NVP-DPP728, 8c) to its follow-up, 1-[[(3-hydroxy-1-adamantyl) amino]acetyl]-2-cyano-(S)-pyrrolidine (NVP-LAF237, 12j). The pharmacological profile of 12j in obese Zucker fa/fa rats along with pharmacokinetic profile comparison of 8c and 12j in normal cynomolgus monkeys is discussed. The results suggest that 12j is a potent, stable, selective DPP-IV inhibitor possessing excellent oral bioavailability and potent antihyperglycemic activity with potential for once-a-day administration.
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Truncated GLP-1 (proglucagon 78?107-amide) inhibits gastric and pancreatic functions in man
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Glucagon-like peptide-1 promotes islet cell growth and inhibits apoptosis in Zucker diabetic rats
Farilla, L., Hui, H., Bertolotto, C., Kang, E., Bulotta, A., Di Mario, U., & Perfetti, R. (2002) · Endocrinology · doi:10.1210/en.2002-220405 · Cited by 502
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Drucker, D. J., & Nauck, M. A. (2006) · The Lancet · doi:10.1016/s0140-6736(06)69705-5 · Cited by 3,896
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
Ahrén, B., Landin-Olsson, M., Jansson, P.-A., Svensson, M., Holmes, D., & Schweizer, A. (2004) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2003-031907 · Cited by 710
Ahrén, B., Gomis, R., Standl, E., Mills, D., & Schweizer, A. (2004) · Diabetes Care · doi:10.2337/diacare.27.12.2874 · Cited by 487
The Metabolic Serine Hydrolases and Their Functions in Mammalian Physiology and Disease
Long, J. Z., & Cravatt, B. F. (2011) · Chemical Reviews · doi:10.1021/cr200075y · Cited by 425
Metadata
- Authors
- Villhauer, E. B., Brinkman, J. A., Naderi, G. B., Burkey, B. F., Dunning, B. E., Prasad, K., Mangold, B. L., Russell, M. E., & Hughes, T. E.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2003-05-24
- Volume
- 46
- Issue
- 13
- Pages
- 2774-2789
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1993287695
- Cited by
- 613
- References
- 6
- FWCI
- 20.83
- Type
- journal article
- Language
- en
- Open access
- green
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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