- Discovery of S1P agonists with a dihydronaphthalene scaffold.
Discovery of S1P agonists with a dihydronaphthalene scaffold.
Bioorganic & medicinal chemistry letters (2011-06-07)
Haruto Kurata, Kensuke Kusumi, Kazuhiro Otsuki, Ryo Suzuki, Masakuni Kurono, Yuka Takada, Hiroki Shioya, Takaki Komiya, Hirotaka Mizuno, Takeji Ono, Hiroshi Hagiya, Masashi Minami, Shinji Nakade, Hiromu Habashita
PMID21641216
摘要
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.