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Synthesis and Biological Activity of an Azido Derivative of Paclobutrazol an Inhibitor of Gibberellin Biosynthesis

机译:多效唑生物合成抑制剂多效唑的叠氮衍生物的合成及生物活性

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摘要

A photolabile azido derivative of the kaurene oxidase inhibitor 1-(4-chlorophenyl)-4,4-dimethyl-2-(1,2,4-triazol-l-yl) pentan-3-ol (paclobutrazol) has been synthesized for use as a photoaffinity labeling agent. The compound was tested as an inhibitor of the oxidation of ent-kaurene catalyzed by cell-free preparations from endosperm of Cucurbita maxima. The I50 of the azido derivative was 9.5 nanomolar, which compares well with that of paclobutrazol (6.3 nanomolar in our measurements). The azido compound bound to Cytochrome P-450 in microsomes from Cucurbita maxima, and induced a Type II spectral change, with an apparent binding constant of 0.24±0.04 micromolar.
机译:合成了月桂烯氧化酶抑制剂1-(4-氯苯基)-4,4-二甲基-2-(1,2,4-三唑-1-基)戊三醇(paclobutrazol)的光不稳定叠氮基衍生物用作光亲和标记剂。测试了该化合物作为由无花南瓜胚乳的无细胞制剂催化的丁香酮氧化的抑制剂。叠氮基衍生物的I50为9.5纳摩尔,与多效唑(在我们的测量中为6.3纳摩尔)相当。叠氮基化合物与最大南瓜属的微粒体中的细胞色素P-450结合,并诱导II型光谱变化,表观结合常数为0.24±0.04微摩尔。

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