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OALib Journal期刊
ISSN: 2333-9721
费用：99美元
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新型5-ht/ne再摄取双重抑制剂的设计、合成及其初步的药理学评价
, PP. 1148-1155
Keywords: 5-羟基色胺,去甲肾上腺素,骨架迁越,双重再摄取抑制剂
Abstract:
本文基于已有的先导结构,结合前期已建立的药效团模型,利用骨架迁越的策略设计并合成两类全新结构类型的异吲哚啉类化合物,通过1hnmr、hr-ms对化合物结构进行了确证,完成了初步的药理活性评价。结果显示,这些化合物均有不同程度的5-ht再摄取抑制活性和ne再摄取抑制活性,其中化合物i-3显示出较强的5-ht再摄取抑制活性和ne再摄取抑制活性,并且在整体动物抗抑郁药效学实验中表现出明确的抗抑郁效果,以及较低的毒副作用,值得进一步研究。
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