Discovery of Highly Potent Dual CysLT(1) and CysLT(2) Antagonist

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))...

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Bibliographic Details
Published inACS medicinal chemistry letters Vol. 5; no. 11; pp. 1230 - 1234
Main Authors Itadani, Satoshi, Takahashi, Shinya, Ima, Masaki, Sekiguchi, Tetsuya, Fujita, Manabu, Nakayama, Yoshisuke, Takeuchi, Jun
Format Journal Article
LanguageEnglish
Published WASHINGTON Amer Chemical Soc 01.11.2014
Subjects
Chemistry, Medicinal
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
CYSTEINYL-LEUKOTRIENE RECEPTOR
dual antagonist
CELLS
Cysteinyl leukotrienes
LTE4
asthma
ASTHMATIC-PATIENTS
CysLT
EXPRESSION
DERIVATIVES
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Summary: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml500298y