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N-芳基2-芳氧基乙酰胺是一类新型的脂肪酸酰胺水解酶(FAAH)抑制剂。
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2017-01-25 , DOI: 10.1080/14756366.2016.1265520 Naresh Sunduru 1 , Mona Svensson 2 , Mariateresa Cipriano 2 , Sania Marwaha 1 , C David Andersson 1 , Richard Svensson 3 , Christopher J Fowler 2 , Mikael Elofsson 1
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2017-01-25 , DOI: 10.1080/14756366.2016.1265520 Naresh Sunduru 1 , Mona Svensson 2 , Mariateresa Cipriano 2 , Sania Marwaha 1 , C David Andersson 1 , Richard Svensson 3 , Christopher J Fowler 2 , Mikael Elofsson 1
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脂肪酸酰胺水解酶(FAAH)是开发用于治疗神经系统疾病的药物的有希望的目标。为了寻找新的FAAH抑制剂,我们确定了2g 2-(4-环己基苯氧基)-N-(3-(恶唑并[4,5-b]吡啶-2-基)苯基)乙酰胺,IC50为2.6 µM,开发有效的FAAH抑制剂的化学起点。初步的逐线优化得到2-i-(4-phenylphenoxy)-N-(3-(oxazolo [4,5-b] pyridin-2-yl)phenyl)乙酰胺4i,IC50为0.35 µM。
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更新日期:2017-01-23
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