Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 11, Pages 1230-1234Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500298y
Keywords
Cysteinyl leukotrienes; CysLT(1); CysLT(2); dual antagonist; asthma
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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.
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