Discovery of a novel class of zwitterionic, potent, selective and orally active S1P1 direct agonists

被引：4

作者：

Aguilar, Nuria ^{[1
]}

Mir, Marta ^{[1
]}

Grima, Pedro M. ^{[2
]}

Lopez, Manel ^{[1
]}

Segarra, Victor ^{[1
]}

Esteban, Laia ^{[3
]}

Moreno, Imma ^{[1
]}

Godessart, Nuria ^{[1
]}

Tarrason, Gema ^{[1
]}

Domenech, Teresa ^{[1
]}

Vilella, Dolors ^{[1
]}

Armengol, Clara ^{[1
]}

Cordoba, Monica ^{[1
]}

Sabate, Mar ^{[1
]}

Casals, Daniel ^{[1
]}

Dominguez, Maria ^{[1
]}

机构：

[1] Labs Almirall SA, Almirall Res Ctr, E-08980 Barcelona, Spain

[2] R&D&I Ctr, Ferrer Grp, E-08028 Barcelona, Spain

[3] Dukechem, E-08799 Barcelona, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 24期

关键词：

RECEPTOR AGONISTS; ENCEPHALOMYELITIS; FTY720;

D O I：

10.1016/j.bmcl.2012.09.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural-activity relationships were developed to yield compounds with good selectivity and excellent in vivo efficacy in rat models. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7672 / 7676

页数：5

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