The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Open accessAbstract
Efforts to further elucidate structure-activity relationships (SAR) within our previously disclosed series of beta-quaternary amino acid linked l-cis-4,5-methanoprolinenitrile dipeptidyl peptidase IV (DPP-IV) inhibitors led to the investigation of vinyl substitution at the beta-position of alpha-cycloalkyl-substituted glycines. Despite poor systemic exposure, vinyl-substituted compounds showed extended duration of action in acute rat ex vivo plasma DPP-IV inhibition models. Oxygenated putative metabolites were prepared and were shown to exhibit the potency and extended duration of action of their precursors in efficacy models measuring glucose clearance in Zucker(fa/fa) rats. Extension of this approach to adamantylglycine-derived inhibitors led to the discovery of highly potent inhibitors, including hydroxyadamantyl compound BMS-477118 (saxagliptin), a highly efficacious, stable, and long-acting DPP-IV inhibitor, which is currently undergoing clinical trials for treatment of type 2 diabetes.
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Cites
Kieffer, T. J., McIntosh, C. H., & Pederson, R. A. (1995) · Endocrinology · doi:10.1210/endo.136.8.7628397 · Cited by 1,124
The Multiple Actions of GLP-1 on the Process of Glucose-Stimulated Insulin Secretion
MacDonald, P. E., El-kholy, W., Riedel, M. J., Salapatek, A. M. F., Light, P. E., & Wheeler, M. B. (2002) · Diabetes · doi:10.2337/diabetes.51.2007.s434 · Cited by 590
Drucker, D. J. (2003) · Endocrinology · doi:10.1210/en.2003-1147 · Cited by 274
Cited by
Drucker, D. J., & Nauck, M. A. (2006) · The Lancet · doi:10.1016/s0140-6736(06)69705-5 · Cited by 3,896
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
DeFronzo, R. A., Hissa, M. N., Garber, A. J., Luiz Gross, J., Yuyan Duan, R., Ravichandran, S., Chen, R. S., & for the Saxagliptin 014 Study Group (2009) · Diabetes Care · doi:10.2337/dc08-1984 · Cited by 416
Dipeptidyl peptidase 4 inhibitors in the treatment of type 2 diabetes mellitus
Deacon, C. F. (2020) · Nature Reviews Endocrinology · doi:10.1038/s41574-020-0399-8 · Cited by 398
BARNETT, A. (2006) · International Journal of Clinical Practice · doi:10.1111/j.1742-1241.2006.01178.x · Cited by 391
Metadata
- Authors
- Augeri, D. J., Robl, J. A., Betebenner, D. A., Magnin, D. R., Khanna, A., Robertson, J. G., Wang, A., Simpkins, L. M., Taunk, P., Huang, Q., Han, S.-P., Abboa-Offei, B., Cap, M., Xin, L., Tao, L., Tozzo, E., Welzel, G. E., Egan, D. M., Marcinkeviciene, J., Chang, S. Y., Biller, S. A., Kirby, M. S., Parker, R. A., & Hamann, L. G.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-06-24
- Volume
- 48
- Issue
- 15
- Pages
- 5025-5037
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2012437459
- Cited by
- 624
- References
- 3
- FWCI
- 16.60
- 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).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
