N-芳基2-芳氧基乙酰胺作为一类新型脂肪酸酰胺水解酶（FAAH）抑制剂。
N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors.
作者信息
Sunduru Naresh, Svensson Mona, Cipriano Mariateresa, Marwaha Sania, Andersson C David, Svensson Richard, Fowler Christopher J, Elofsson Mikael
机构信息
a Department of Chemistry , Umeå University , Umeå , Sweden.
b Department of Pharmacology and Clinical Neuroscience , Umeå University , Umeå , Sweden.
出版信息
J Enzyme Inhib Med Chem. 2017 Dec;32(1):513-521. doi: 10.1080/14756366.2016.1265520.
Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC of 2.6 µM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC of 0.35 µM.
脂肪酸酰胺水解酶（FAAH）是开发治疗神经疾病药物的一个有前景的靶点。为了寻找新的FAAH抑制剂，我们确定了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（4g），其IC50为2.6 μM，作为开发强效FAAH抑制剂的化学起始点。初步的从苗头化合物到先导化合物的优化产生了2-(4-苯基苯氧基)-N-(3-(恶唑并[4,5-b]吡啶-2-基)苯基)乙酰胺（4i），其IC50为0.35 μM。
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