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Development of 3,4-dihydro-2H-benzo[1,4]oxazine derivatives as dual thromboxane A2 receptor antagonists and prostacyclin receptor agonists.

作者信息

Ohno Michihiro, Tanaka Yoichiro, Miyamoto Mitsuko, Takeda Takahiro, Hoshi Kazuhiro, Yamada Naohiro, Ohtake Atsushi

机构信息

Pharmaceutical Research Laboratories, Toray Industries, Inc. 1,111 Tebiro, Kamakura, Kanagawa 248-8555, Japan.

出版信息

Bioorg Med Chem. 2006 Mar 15;14(6):2005-21. doi: 10.1016/j.bmc.2005.10.050. Epub 2005 Nov 16.

DOI:10.1016/j.bmc.2005.10.050
PMID:16297632
Abstract

We discovered a novel series of 3,4-dihydro-2H-benzo[1,4]oxazin-8-yloxyacetic acid derivatives as potent dual-acting agents to block the TXA2 receptor and to activate the PGI2 receptor. We report the synthesis, structure-activity relationship, and in vitro, ex vivo, and in vivo pharmacology of this series of compounds. 4-[2-(1,1-Diphenylethylsulfanyl)ethyl]-3,4-dihydro-2H-benzo[1,4]oxazin-8-yloxyacetic acid N-methyl-D-glucamine salt (7) is a promising candidate for a novel treatment in the anti-thrombotic and the cardiovascular fields avoiding hypotensive side effects.

摘要

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