949114-22-1Relevant articles and documents
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis
Park, Sun Jun,Yeon, Seul Ki,Kim, Yoowon,Kim, Hyeon Jeong,Kim, Siwon,Kim, Jushin,Choi, Ji Won,Kim, Byungeun,Lee, Elijah Hwejin,Kim, Rium,Seo, Seon Hee,Lee, Jaeick,Kim, Jun Woo,Lee, Ha-Yeon,Hwang, Hayoung,Bahn, Yong-Sun,Cheong, Eunji,Park, Jong-Hyun,Park, Ki Duk
supporting information, p. 3539 - 3562 (2022/02/10)
The sphingosine-1-phosphate-1 (S1P1) receptor agonists have great potential for the treatment of multiple sclerosis (MS) because they can inhibit lymphocyte egress through receptor internalization. We designed and synthesized triazole and isoxazoline derivatives to discover a novel S1P1agonist for MS treatment. Of the two scaffolds, the isoxazoline derivative was determined to have excellent in vitro efficacy and drug-like properties. Among them, compound 21l was found to have superior drug-like properties as well as excellent in vitro efficacies (EC50= 7.03 nM in β-arrestin recruitment and EC50= 11.8 nM in internalization). We also confirmed that 21l effectively inhibited lymphocyte egress in the peripheral lymphocyte count test and significantly improved the clinical score in the experimental autoimmune encephalitis MS mouse model.
Copper-catalyzed domino route to natural nostoclides and analogues: A total synthesis of nostoclides i and II
Ngi, Samuel Inack,Petrignet, Julien,Duwald, Romain,El Hilali, El Mostafa,Abarbri, Mohamed,Duchêne, Alain,Thibonnet, Jér?me
, p. 2936 - 2941 (2014/03/21)
An original and convenient domino route to natural nostoclides I and II has been developed using a two-step sequence consisting of a copper-cat-alyzed tandem reaction associated with Suzuki cross-coupling. The methodology employed for this total synthesis appeared to be an interesting and suffi-ciently flexible tool to allow the synthesis of numer-ous analogues of these nostoclides.
