Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist

Discovery of Highly Potent Dual CysLT1 and CysLT2 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 CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respective...

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Veröffentlicht in:ACS medicinal chemistry letters 2014-11, Vol.5 (11), p.1230-1234
Hauptverfasser: Itadani, Satoshi, Takahashi, Shinya, Ima, Masaki, Sekiguchi, Tetsuya, Fujita, Manabu, Nakayama, Yoshisuke, Takeuchi, Jun
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml500298y