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Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.

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 ?M (CysLT1) and 0.00087 ?M (CysLT2), respectively.

SUBMITTER: Itadani S

PROVIDER: S-EPMC4233365 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature

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Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.

Itadani Satoshi S Takahashi Shinya S Ima Masaki M Sekiguchi Tetsuya T Fujita Manabu M Nakayama Yoshisuke Y Takeuchi Jun J

ACS medicinal chemistry letters 20141006 11

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. ...[more]

PMID: 25408836

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