2. Academic Validation
  3. Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist

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

Affiliation

  • 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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