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Investigation of thiazolyl–benzothiophenamides as potential agents for African sleeping sickness
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-09-23 , DOI: 10.1039/d0md00277a
Ronald W Brown 1 , Ashraf M Abdel-Megeed 1 , Paul A Keller 1 , Amy J Jones 2 , Melissa L Sykes 2 , Marcel Kaiser 3, 4 , Jonathan B Baell 5 , Vicky M Avery 2 , Christopher J T Hyland 1
Affiliation  

African sleeping sickness is a potentially fatal neglected disease affecting sub-Saharan Africa. High-throughput screening identified the thiazolyl–benzothiophenamide 1 to be active against the causative parasite, Trypanosoma brucei. This work establishes structure–activity relationships of 1, guiding the design of second generation derivatives. After screening against the clinically relevant species T. b. rhodesiense, the derivative 16 was identified as a suitable candidate for further investigation.

中文翻译:


噻唑基苯并噻吩酰胺作为非洲昏睡病潜在药物的研究



非洲昏睡病是一种可能致命的被忽视的疾病,影响撒哈拉以南非洲地区。高通量筛选发现噻唑基苯并噻吩酰胺1对致病寄生虫布氏锥虫具有活性。这项工作建立了1的构效关系,指导第二代衍生物的设计。针对临床相关物种T. b.进行筛选后。 rhodesense 中,衍生物16被确定为进一步研究的合适候选者。
更新日期:2020-11-03
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