Synthesis of a C1-C23 fragment of the archazolids and evidence for V-ATPase but not COX inhibitory activity.

Synthesis of a C1-C23 fragment of the archazolids and evidence for V-ATPase but not COX inhibitory activity.
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archazolid 的 C1-C23 片段的合成以及 V-ATP 酶而非 COX 抑制活性的证据。

DOI:
10.1055/s-0036-1588413
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发表时间:
2017
期刊:
Synlett : accounts and rapid communications in synthetic organic chemistry
影响因子:
--
通讯作者:
Spiegel,PClint
Spiegel,PClint
中科院分区:
--
文献类型:
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作者:
O'Neil,GregoryW;Craig,AlexanderM;Williams,JohnR;Young,JeffreyC;Spiegel,PClint

文献摘要

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基于高产率的Stille偶联反应,完成了一个含C1-C23残基的咪唑类化合物的聚合合成,构建了取代的Z,Z,E-共轭三烯。去除保护基后,所得四醇显示出抑制空泡型ATP酶(V-ATP酶)但不抑制环氧合酶(考克斯)抑制活性的证据。
A convergent synthesis of a C1–C23fragment of the archazolids has been completed based on a high-yielding Stille coupling to construct the substitutedZ,Z,E-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.