Structure–activity relationship studies of S1P agonists with a dihydronaphthalene scaffold

…, H Hagiya, M Minami, S Nakade, H Habashita

文献索引：Kurata, Haruto; Kusumi, Kensuke; Otsuki, Kazuhiro; Suzuki, Ryo; Kurono, Masakuni; Tokuda, Natsuko; Takada, Yuka; Shioya, Hiroki; Mizuno, Hirotaka; Komiya, Takaki; Ono, Takeji; Hagiya, Hiroshi; Minami, Masashi; Nakade, Shinji; Habashita, Hiromu Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 144 - 148

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被引用次数: 11

摘要

Structure–activity relationship (SAR) of sphingosine-1-phosphate receptor agonists with a dihydronaphthalene scaffold was investigated. Compound 1 was modified to improve S1P1 agonistic activity and in vivo peripheral lymphocyte lowering (PLL) activity without impairing selectivity over S1P3 agonistic activity. A detailed SAR study of the terminal lipophilic part revealed that the introduction of substituents on the propylene linker and the terminal ...