The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Discovery of Tofogliflozin, a Novel C-Arylglucoside with an O-Spiroketal Ring System, as a Highly Selective Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes
Open accessAbstract
Inhibition of sodium glucose cotransporter 2 (SGLT2) has been proposed as a novel therapeutic approach to treat type 2 diabetes. In our efforts to discover novel inhibitors of SGLT2, we first generated a 3D pharmacophore model based on the superposition of known inhibitors. A search of the Cambridge Structural Database using a series of pharmacophore queries led to the discovery of an O-spiroketal C-arylglucoside scaffold. Subsequent chemical examination combined with computational modeling resulted in the identification of the clinical candidate 16d (CSG452, tofogliflozin), which is currently under phase III clinical trials.
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Stratton, I. M. (2000) · BMJ · doi:10.1136/bmj.321.7258.405 · Cited by 9,059
Meng, W., Ellsworth, B. A., Nirschl, A. A., McCann, P. J., Patel, M., Girotra, R. N., Wu, G., Sher, P. M., Morrison, E. P., Biller, S. A., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701272q · Cited by 634
Komoroski, B., Vachharajani, N., Feng, Y., Li, L., Kornhauser, D., & Pfister, M. (2009) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.2008.250 · Cited by 396
Glucose dynamics and mechanistic implications of SGLT2 inhibitors in animals and humans
List, J. F., & Whaley, J. M. (2011) · Kidney International · doi:10.1038/ki.2010.512 · Cited by 184
S-1: a promising new oral fluoropyrimidine derivative
Saif, M. W., Syrigos, K. N., & Katirtzoglou, N. A. (2009) · Expert Opinion on Investigational Drugs · doi:10.1517/13543780902729412 · Cited by 101
Cited by
SLC Transporters as Therapeutic Targets: Emerging Opportunities
Lin, L., Yee, S. W., Kim, R. B., & Giacomini, K. M. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4626 · Cited by 835
The modification of natural products for medical use
Guo, Z. (2017) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2016.06.003 · Cited by 328
The utilization of spirocyclic scaffolds in novel drug discovery
Zheng, Y.-J., & Tice, C. M. (2016) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2016.1195367 · Cited by 299
Inhibition of MEK1 signaling pathway in the liver ameliorates insulin resistance
Ueyama, A., Ban, N., Fukazawa, M., Hirayama, T., Takeda, M., Yata, T., Muramatsu, H., Hoshino, M., Yamamoto, M., Matsuo, M., et al. (2016) · Journal of Diabetes Research · doi:10.1155/2016/8264830 · Cited by 7
Metadata
- Authors
- Ohtake, Y., Sato, T., Kobayashi, T., Nishimoto, M., Taka, N., Takano, K., Yamamoto, K., Ohmori, M., Yamaguchi, M., Takami, K., Yeu, S.-Y., Ahn, K.-H., Matsuoka, H., Morikawa, K., Suzuki, M., Hagita, H., Ozawa, K., Yamaguchi, K., Kato, M., & Ikeda, S.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-08-28
- Volume
- 55
- Issue
- 17
- Pages
- 7828-7840
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1982261994
- Cited by
- 174
- References
- 5
- FWCI
- 10.81
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Discovery of Tofogliflozin, a Novel C-Arylglucoside with an O-Spiroketal Ring System, as a Highly Selective Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes. https://app.cochat.ai/papers/10.1021/jm300884k
- The paper
- Ohtake, Y., Sato, T., Kobayashi, T., Nishimoto, M., Taka, N., Takano, K., Yamamoto, K., Ohmori, M., Yamaguchi, M., Takami, K., Yeu, S.-Y., Ahn, K.-H., Matsuoka, H., Morikawa, K., Suzuki, M., Hagita, H., Ozawa, K., Yamaguchi, K., Kato, M., & Ikeda, S. (2012). Discovery of Tofogliflozin, a Novel C-Arylglucoside with an O-Spiroketal Ring System, as a Highly Selective Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm300884k
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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.
