Design,Synthesis and Biological Evaluation of Benzimidazole Derivatives as H3 Receptor Antagonists a

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户:astolzq
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  Histamine H3 receptor(H3R) is a presynaptic GPCR receptor regulating the synthesis and release of histamine as well as other important neurotransmitters,such as ACh,5-HT and DA.Development of H3R antagonists has been proved to be an effective strategy in treating Alzheimers Disease(AD) with five drug candidates are currently in clinical trial.β-amyloid(Aβ) aggregation and deposition is believed to bear central role in the pathogenesis of AD.Recent evidence indicated that excess metal ion in brain(Fe2+,Cu2+,Zn2+) may promote the aggregation of Aβ.Therefore,decreasing the level of metal ions in brain by using metal chelator represents another rational therapeutic approach for treating AD.
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