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阿扎唑类化合物C-C片段的合成以及V-ATP酶抑制活性而非COX抑制活性的证据

Synthesis of a C-C fragment of the archazolids and evidence for V-ATPase but not COX inhibitory activity.

作者信息

O'Neil Gregory W, Craig Alexander M, Williams John R, Young Jeffrey C, Spiegel P Clint

机构信息

Department of Chemistry, Western Washington University, Bellingham, WA, USA.

Department of Biology, Western Washington University, Bellingham, WA, USA.

出版信息

Synlett. 2017 Jun;28(9):1101-1105. doi: 10.1055/s-0036-1588413. Epub 2017 Feb 8.

Abstract

A convergent synthesis of a C-C fragment of the archazolids has been completed based on a high yielding Stille coupling to costruct the substituted ,,-conjugated triene. After removal of the protecting groups, the resulting tetrol exhibited evidence for inhibition of the vacuolar-type ATPase (V-ATPase) but not cyclooxygenase (COX) inhibitory activity.

摘要

基于高产率的Stille偶联反应完成了阿扎唑类化合物碳-碳片段的汇聚合成,以构建取代的、、共轭三烯。在除去保护基后,所得的四醇显示出抑制液泡型ATP酶(V-ATP酶)的证据,但没有环氧合酶(COX)抑制活性。

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