3-芳基-3-唑基丙-1-胺类化合物的合成及作为选择性三胺摄取抑制剂的药理学评价。
Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
机构信息
Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. doi: 10.1016/j.bmcl.2010.07.021. Epub 2010 Aug 17.
PMID:20724153
Abstract
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In vivo models were used to evaluate the compound 19r for antidepressive, anxiolytic, and analgesic activity.
摘要
合成了一系列 3-芳基-3-唑基丙-1-胺，并对其抑制单胺再摄取的能力进行了筛选。描述了具有纳摩尔效力、良好的人体外微粒体稳定性和低药物相互作用潜力的类似物。使用体内模型评估了化合物 19r 的抗抑郁、抗焦虑和镇痛活性。
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