Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)

被引：16

作者：

Lanman, Brian A. ^{[1
]}

Cee, Victor J. ^{[1
]}

Cheruku, Srinivasa R. ^{[2
]}

Frohn, Mike ^{[1
]}

Golden, Jennifer ^{[1
]}

Lin, Jian ^{[2
]}

Lobera, Mercedes ^{[2
]}

Marantz, Yael ^{[2
]}

Muller, Kristine M. ^{[1
]}

Neira, Susana C. ^{[1
]}

Pickrell, Alexander J. ^{[1
]}

Rivenzon-Segal, Dalia ^{[2
]}

Schutz, Nili ^{[2
]}

Sharadendu, Anurag ^{[2
]}

Yu, Xiang ^{[2
]}

Zhang, Zhaoda ^{[2
]}

Buys, Janet ^{[1
]}

Fiorino, Mike ^{[1
]}

Gore, Anu ^{[1
]}

Horner, Michelle ^{[1
]}

Itano, Andrea ^{[1
]}

McElvain, Michele ^{[1
]}

Middleton, Scot ^{[1
]}

Schrag, Michael ^{[1
]}

Vargas, Hugo M. ^{[1
]}

Xu, Han ^{[1
]}

Xu, Yang ^{[1
]}

Zhang, Xuxia ^{[1
]}

Siu, Jerry ^{[1
]}

Buerli, Roland W. ^{[1
]}

机构：

[1] Amgen Inc, Thousand Oaks, CA 91320 USA

[2] EPIX Pharmaceut Inc, Wellesley Hills, MA 02481 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2011年 / 2卷 / 02期

关键词：

Sphingosine-1-phosphate receptor; S1P(1); agonist; inflammation; lymphocyte; SPHINGOSINE 1-PHOSPHATE RECEPTOR; RELAPSING MULTIPLE-SCLEROSIS; LYMPHOID ORGANS; ORAL FINGOLIMOD; HEART-RATE; FTY720; RATS; IMMUNOSUPPRESSANT; SPHINGOLIPIDS; EXPRESSION;

D O I：

10.1021/ml100228m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Optimization of a benzofuranyl SIP, agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)-azetidine-3-carboxylic acid (14), a potent SIP, agonist with minimal activity at S1P(3). Dosed orally at 0.3 mg/kg, 14 significantly reduced blood lymphocyte counts 24 h postdose and attenuated a delayed type hypersensitivity (DTH) response to antigen challenge.

引用

页码：102 / 106

页数：5

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