鉴定和开发 1,4-苯并二氮杂卓-2-酮和喹唑啉-2,4-二酮支架作为 HAT 的亚毫摩尔抑制剂。
Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT.
机构信息
Strathclyde Institute for Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0RE, UK.
出版信息
Bioorg Med Chem. 2012 Oct 15;20(20):6019-33. doi: 10.1016/j.bmc.2012.08.049. Epub 2012 Aug 31.
PMID:22985960
Abstract
A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 μM. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds.
摘要
已经合成了一个 1,4-苯并二氮杂䓬文库，并对其进行了抗非洲人体锥虫病（HAT）的致病寄生虫——布氏锥虫的活性评估。这些衍生物中最有效的一种的 MIC 值为 0.97 μM。在此，我们报告上述化合物的设计、合成和生物学评价。
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