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Synthesis and Evaluation of Serinolamide Derivatives as Sphingosine-1-Phosphate-1 (S1P1) Receptor Agonists.

ABSTRACT: Sphingosine-1-phosphate-1 (S1P1) receptor agonists are well-known drugs for treating multiple sclerosis (MS) caused by autoreactive lymphocytes that attack the myelin sheath. Therefore, an effective therapeutic strategy is to reduce the lymphocytes in the blood by inducing S1P1 receptor internalization. We synthesized serinolamide A, a natural product of the sea, and performed S1P1 receptor internalization assay to evaluate functionally antagonistic S1P1 receptor agonist activity. In order to synthesize derivatives with better efficacy than serinolamide A and B, new derivatives were synthesized by introducing the phenyl ring moiety of fingolimod. Among them, compounds 19 and 21 had superior S1P1 agonistic effects to serinolamide. We also confirmed that compound 19 effectively inhibited lymphocyte outflow in peripheral lymphocyte count (PLC) assay.

SUBMITTER: Park SJ 

PROVIDER: S-EPMC9101607 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature

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Synthesis and Evaluation of Serinolamide Derivatives as Sphingosine-1-Phosphate-1 (S1P<sub>1</sub>) Receptor Agonists.

Park Sun Jun SJ   Kim Jushin J   Kim Jaehwan J   Kim Yoowon Y   Lee Elijah Hwejin EH   Kim Hyeon Jeong HJ   Kim Siwon S   Kim Byungeun B   Kim Rium R   Choi Ji Won JW   Park Jong-Hyun JH   Park Ki Duk KD  

Molecules (Basel, Switzerland) 20220428 9

Sphingosine-1-phosphate-1 (S1P<sub>1</sub>) receptor agonists are well-known drugs for treating multiple sclerosis (MS) caused by autoreactive lymphocytes that attack the myelin sheath. Therefore, an effective therapeutic strategy is to reduce the lymphocytes in the blood by inducing S1P<sub>1</sub> receptor internalization. We synthesized serinolamide A, a natural product of the sea, and performed S1P<sub>1</sub> receptor internalization assay to evaluate functionally antagonistic S1P<sub>1</su  ...[more]

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