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具有半胱氨酰白三烯受体2拮抗活性的3-乙酰乙酰氨基苯并[b]呋喃衍生物的制备

Preparation of 3-acetoacetylaminobenzo[b]furan derivatives with cysteinyl leukotriene receptor 2 antagonistic activity.

作者信息

Tsuji Eriko, Ando Kumiko, Kunitomo Jun-ichi, Yamashita Masayuki, Ohta Shunsaku, Kohno Shigekatsu, Ohishi Yoshitaka

机构信息

School of Pharmaceutical Sciences, Mukogawa-Women's University, 11-68 Koshien Kyuban-cho, Nishinomiya 663-8179, Japan.

出版信息

Org Biomol Chem. 2003 Sep 21;1(18):3139-41. doi: 10.1039/b307468d.

DOI:10.1039/b307468d
PMID:14527142
Abstract

Novel 3-acetoacetylaminobenzo[b]furan derivatives with a modified triene system at the 3-position were prepared through acylation of the 3-aminobenzo[b]furans with 5-methylisoxazole-4-carboxylic acid chloride followed by basic cleavage of the isoxazole ring and several of these compounds showed moderate cysteinyl leukotriene receptor 2 antagonistic activity.

摘要

通过用5-甲基异恶唑-4-羧酸氯对3-氨基苯并[b]呋喃进行酰化反应,然后对异恶唑环进行碱性裂解,制备了在3位具有修饰三烯系统的新型3-乙酰乙酰氨基苯并[b]呋喃衍生物,其中几种化合物表现出中等程度的半胱氨酰白三烯受体2拮抗活性。

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Preparation of 3-acetoacetylaminobenzo[b]furan derivatives with cysteinyl leukotriene receptor 2 antagonistic activity.具有半胱氨酰白三烯受体2拮抗活性的3-乙酰乙酰氨基苯并[b]呋喃衍生物的制备
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Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.高效双半胱氨酰白三烯1和半胱氨酰白三烯2拮抗剂的发现。
ACS Med Chem Lett. 2014 Oct 6;5(11):1230-4. doi: 10.1021/ml500298y. eCollection 2014 Nov 13.