Discovery of S1P agonists with a dihydronaphthalene scaffold

Autor:	Takeji Ono, Kazuhiro Otsuki, Ryo Suzuki, Masakuni Kurono, Takaki Komiya, Hiroki Shioya, Masashi Minami, Hirotaka Mizuno, Yuka Takada, Haruto Kurata, Hiroshi Hagiya, Hiromu Habashita, Shinji Nakade, Kensuke Kusumi
Rok vydání:	2011
Předmět:	Agonist Propanols medicine.drug_class Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science CHO Cells Naphthalenes Biochemistry Chemical synthesis Mice Structure-Activity Relationship Cricetulus Sphingosine In vivo Cricetinae Drug Discovery medicine Animals Humans Structure–activity relationship Lymphocytes Receptor Molecular Biology G protein-coupled receptor Molecular Structure Fingolimod Hydrochloride Chemistry organic chemicals Organic Chemistry In vitro Receptors Lysosphingolipid Propylene Glycols Molecular Medicine lipids (amino acids peptides and proteins) Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:3885-3889
ISSN:	0960-894X
Popis:	Structure-activity relationship of sphingosine-1-phosphate receptor agonists was examined. Cinnamyl derivative 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Dihydronaphthalene derivative 10d was identified as a potent S1P(1) receptor agonist with high selectivity against S1P(3) and enhanced efficacy in lowering peripheral lymphocyte counts in mice.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b0ea6076a0e05454b8edfc392d3ac65 https://doi.org/10.1016/j.bmcl.2011.05.029 Zobrazit plný text záznamu Full Text from ScienceDirect