Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist

被引：12

作者：

Itadani, Satoshi ^{[1
]}

Takahashi, Shinya ^{[1
]}

Ima, Masaki ^{[1
]}

Sekiguchi, Tetsuya ^{[1
]}

Fujita, Manabu ^{[2
]}

Nakayama, Yoshisuke ^{[1
]}

Takeuchi, Jun ^{[1
]}

机构：

[1] Ono Pharmaceut Co Ltd, Med Chem Res Labs, Shimamoto, Osaka 6188585, Japan

[2] Ono Pharmaceut Co Ltd, Dept Biol & Pharmacol, Shimamoto, Osaka 6188585, Japan

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2014年 / 5卷 / 11期

关键词：

Cysteinyl leukotrienes; CysLT(1); CysLT(2); dual antagonist; asthma; CYSTEINYL-LEUKOTRIENE RECEPTOR; ASTHMATIC-PATIENTS; EXPRESSION; CELLS; DERIVATIVES; LTE4;

D O I：

10.1021/ml500298y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The benzoxazine derivative, (2S)-4-(3-carboxypropyl)-8-{[4-(4-phenylbutoxy)benzoyl]amino}-3,4-dihydro-2H-1,4-benzoxazine-2-carboxylic acid (19, ONO-2050297), was identified as the first potent dual CysLT(1) and CysLT(2) antagonist with IC50 values of 0.017 mu M (CysLT(1)) and 0.00087 mu M (CysLT(2)), respectively.

引用

页码：1230 / 1234

页数：5

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