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4-苯甲酰基-1,2,3-三唑-N-乙酸和4-苄基-1,2,3-三唑-N-乙酸,前列腺素合成的体外抑制剂。

4-Benzoyl- and 4-benzyl-1,2,3-triazol-N-acetic acids, in vitro inhibitors of the prostaglandin synthesis.

作者信息

Biagi G, Ferretti M, Livi O, Scartoni V, Lucacchini A, Mazzoni M

出版信息

Farmaco Sci. 1986 May;41(5):388-400. doi: 10.1002/chin.198646225.

Abstract

Several 4-benzoyl- and 4-benzyl-1,2,3-triazol-N-acetic derivatives were synthesized and tested. The compounds were prepared by nucleophilic substitution, 1,3-dipolar cycloaddition and usual functional group conversion reactions. Numerous derivatives were evaluated in vitro for their ability to inhibit the prostaglandin synthesis and to displace labelled [14C]indomethacin from bovine vesicular gland microsomes. Some compounds showed biological activity.

摘要

合成并测试了几种4-苯甲酰基-和4-苄基-1,2,3-三唑-N-乙酸衍生物。这些化合物通过亲核取代、1,3-偶极环加成和常规官能团转化反应制备。对众多衍生物进行了体外评估,以检测它们抑制前列腺素合成以及从牛精囊微粒体中置换标记的[14C]吲哚美辛的能力。一些化合物显示出生物活性。

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