基于查尔酮的芳氧基丙醇胺作为潜在的抗高血糖药物。
Chalcone based aryloxypropanolamines as potential antihyperglycemic agents.
作者信息
Shukla Poonam, Singh Amar Bahadur, Srivastava Arvind Kumar, Pratap Ram
机构信息
Central Drug Research Institute, Lucknow, India.
出版信息
Bioorg Med Chem Lett. 2007 Feb 1;17(3):799-802. doi: 10.1016/j.bmcl.2006.10.068. Epub 2006 Oct 27.
A series of chalcone based aryloxypropanolamines were synthesized and evaluated for their antihyperglycemic activity in SLM and STZ rat models. Most of the compounds exhibited moderate to good activity ranging from 6.5% to 31.1% in SLM and 8.3% to 22.6% in STZ models, respectively. The most potent compound 5 g exhibited glucose lowering of 26.7% in SLM and 22.6% in STZ models. A definite structure-activity relationship was observed while varying the nature as well as the position of the amine in ring B.
合成了一系列基于查尔酮的芳氧基丙醇胺，并在链脲佐菌素（SLM）和链脲佐菌素（STZ）大鼠模型中评估了它们的抗高血糖活性。大多数化合物在SLM模型中表现出中等至良好的活性，范围为6.5%至31.1%，在STZ模型中为8.3%至22.6%。最有效的化合物5g在SLM模型中使血糖降低26.7%，在STZ模型中降低22.6%。在改变环B中胺的性质和位置时，观察到了明确的构效关系。
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