设计和合成新型人犬尿氨酸氨基转移酶-I 抑制剂。
Design and synthesis of novel inhibitors of human kynurenine aminotransferase-I.
机构信息
Faculty of Pharmacy A15, The University of Sydney, Sydney, NSW 2006, Australia.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1579-81. doi: 10.1016/j.bmcl.2011.12.138. Epub 2012 Jan 10.
Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1H-indole-2-carboxylic acid derivatives as synthetically accessible leads for human kynurenine aminotransferase-I (KAT-I) inhibitors. In total, 12 compounds were synthesized and their biological activities were determined using the HPLC-UV based KAT-I inhibition assay. Of the 12 compounds synthesized, 10 were found to inhibit human KAT-I and the most active compound was found to be 5-(2-(4-chlorophenyl) hydrazono)-6-ethoxy-6-oxohexanoic acid (9a) with an IC(50) of 19.8 μM.
在此，我们报告了 6-乙氧基-6-氧代-5-(2-苯腙基)己酸和 3-(2-羧乙基)-1H-吲哚-2-羧酸衍生物，它们是可合成的人犬尿氨酸氨基转移酶-I（KAT-I）抑制剂的先导化合物。总共合成了 12 种化合物，并使用基于 HPLC-UV 的 KAT-I 抑制测定法测定了它们的生物活性。在所合成的 12 种化合物中，有 10 种被发现抑制人 KAT-I，最有效的化合物被发现是 5-(2-(4-氯苯基)腙基)-6-乙氧基-6-氧代己酸（9a），其 IC50 为 19.8 μM。
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