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Bioorg Med Chem Lett. 2011 Mar 1;21(5):1390-3. doi: 10.1016/j.bmcl.2011.01.029. Epub 2011 Jan 11.

Structure-activity relationship studies of sphingosine-1-phosphate receptor agonists with N-cinnamyl-β-alanine moiety.

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1
Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, Mishima, Osaka 618-8585, Japan. h.kurata@ono.co.jp

Abstract

Structure-activity relationship of sphingosine-1-phosphate receptor agonist was examined. In terms of reducing the flexibility of molecule, hit compound 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Novel S1P agonists with cinnamyl scaffold or 1,2,5,6-tetrahydropyridine scaffold were identified.

PMID:
21295477
DOI:
10.1016/j.bmcl.2011.01.029
[Indexed for MEDLINE]
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