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Bioorg Med Chem Lett. 2015 Apr 1;25(7):1479-82. doi: 10.1016/j.bmcl.2015.02.029. Epub 2015 Feb 23.

Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.

Author information

1
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan. Electronic address: kusumi@ono.co.jp.
2
Ono Pharma UK Ltd, MidCity Place, 71 High Holborn, London WC1V 6EA, United Kingdom.
3
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.
4
Head Office, Ono Pharmaceutical Co., Ltd, 8-2, Kyutaromachi 1-chome, Chuo-ku, Osaka 541-8564, Japan.

Abstract

The structure-activity relationships of a novel series of sphingosine-1-phosphate receptor antagonists have been examined in detail. The initial hit compound 1 was modified through synthesis to improve its S1P2 activity. The synthesis of a series of analogs revealed that 1,3-bis(aryloxy)benzene derivatives, as represented by 22, are potent and selective S1P2 antagonists.

KEYWORDS:

Antagonist; G protein-coupled receptors; Sphingosine-1-phosphate receptor 2

PMID:
25746814
DOI:
10.1016/j.bmcl.2015.02.029
[Indexed for MEDLINE]

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