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2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1Receptor Agonists
Open accessAbstract
Sphingosine-1-phosphate (S1P) is a widespread lysophospholipid which displays a wealth of biological effects. Extracellular S1P conveys its activity through five specific G-protein coupled receptors numbered S1P(1) through S1P(5). Agonists of the S1P(1) receptor block the egress of T-lymphocytes from thymus and lymphoid organs and hold promise for the oral treatment of autoimmune disorders. Here, we report on the discovery and detailed structure-activity relationships of a novel class of S1P(1) receptor agonists based on the 2-imino-thiazolidin-4-one scaffold. Compound 8bo (ACT-128800) emerged from this series and is a potent, selective, and orally active S1P(1) receptor agonist selected for clinical development. In the rat, maximal reduction of circulating lymphocytes was reached at a dose of 3 mg/kg. The duration of lymphocyte sequestration was dose dependent. At a dose of 100 mg/kg, the effect on lymphocyte counts was fully reversible within less than 36 h. Pharmacokinetic investigation of 8bo in beagle dogs suggests that the compound is suitable for once daily dosing in humans.
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Cited by
Recent developments and biological activities of thiazolidinone derivatives: A review
Jain, A. K., Vaidya, A., Ravichandran, V., Kashaw, S. K., & Agrawal, R. K. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.03.069 · Cited by 461
Targeting the sphingosine-1-phosphate axis in cancer, inflammation and beyond
Kunkel, G. T., Maceyka, M., Milstien, S., & Spiegel, S. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd4099 · Cited by 434
Experimental Pharmacological Management of Psoriasis
Campione, E., Cosio, T., Di Prete, M., Lanna, C., Dattola, A., & Bianchi, L. (2021) · Journal of Experimental Pharmacology · doi:10.2147/jep.s265632 · Cited by 27
Metadata
- Authors
- Bolli, M. H., Abele, S., Binkert, C., Bravo, R., Buchmann, S., Bur, D., Gatfield, J., Hess, P., Kohl, C., Mangold, C., Mathys, B., Menyhart, K., Müller, C., Nayler, O., Scherz, M., Schmidt, G., Sippel, V., Steiner, B., Strasser, D., Treiber, A., & Weller, T.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-05-27
- Volume
- 53
- Issue
- 10
- Pages
- 4198-4211
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2068857175
- Cited by
- 179
- References
- 0
- FWCI
- 5.08
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: 2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1Receptor Agonists. https://app.cochat.ai/papers/10.1021/jm100181s
- The paper
- Bolli, M. H., Abele, S., Binkert, C., Bravo, R., Buchmann, S., Bur, D., Gatfield, J., Hess, P., Kohl, C., Mangold, C., Mathys, B., Menyhart, K., Müller, C., Nayler, O., Scherz, M., Schmidt, G., Sippel, V., Steiner, B., Strasser, D., . . . Weller, T. (2010). 2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1Receptor Agonists. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm100181s
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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.
