Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist

  • ACS Med Chem Lett. 2014 Oct 6;5(11):1230-4. doi: 10.1021/ml500298y.
Satoshi Itadani  1 ,  Shinya Takahashi  1 ,  Masaki Ima  1 ,  Tetsuya Sekiguchi  1 ,  Manabu Fujita  1 ,  Yoshisuke Nakayama  1 ,  Jun Takeuchi  1
Affiliations
  • 1. Medicinal Chemistry Research Laboratories and Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd. , 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
PMID: 25408836 DOI: 10.1021/ml500298y
Abstract

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 CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.

Keywords
CysLT1; CysLT2; Cysteinyl leukotrienes; asthma; dual antagonist.
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