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首页> 外文期刊>Bioorganic and medicinal chemistry >Novel nitric oxide-releasing isochroman-4-one derivatives: Synthesis and evaluation of antihypertensive activity
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Novel nitric oxide-releasing isochroman-4-one derivatives: Synthesis and evaluation of antihypertensive activity

机译:新型释放一氧化氮的异色满-4-酮衍生物:降压活性的合成和评价

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摘要

By coupling nitric oxide (NO)-donor moieties with a natural antihypertensive product (±)-7,8-dihydroxy-3-methyl-isochroman-4-one [(±)-XJP] and its analogue (±)-XJP-B, a series of novel NO-releasing isochroman-4-one derivatives were designed and synthesized. The NO-releasing assay indicated that compounds Ia, Id, IIIb and IIIe released the maximum amount of NO. The maximum reductions of blood pressure of Ia, IIIb and IIIe in SHRs were nearly 40%, which was obviously superior to that of the lead compounds and comparable to that of reference drug captopril. These results suggested that NO-donoratural product hybrids may provide a promising approach for the discovery of novel antihypertensive agents.
机译:通过将一氧化氮(NO)供体部分与天然降压产物(±)-7,8-二羟基-3-甲基-异色满-4-酮[(±)-XJP]及其类似物(±)-XJP- B,设计并合成了一系列新颖的释放NO的异色满-4-酮衍生物。 NO释放测定表明化合物Ia,Id,IIIb和IIIe释放最大量的NO。 SHRs中Ia,IIIb和IIIe的最大降压幅度接近40%,这明显优于先导化合物,与参考药物卡托普利相当。这些结果表明,NO供体/天然产物杂合体可能为发现新型降压药提供有前途的方法。

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