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Structure–Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-22 , DOI: 10.1021/acsmedchemlett.9b00455 Melissa J Buskes 1 , Monica Clements 1 , Kelly A Bachovchin 1 , Hitesh B Jalani 1 , Allison Leonard 1 , Seema Bag 1 , Dana M Klug 1 , Baljinder Singh 1 , Robert F Campbell 2 , Richard J Sciotti 2 , Nelly El-Sakkary 3 , Conor R Caffrey 3 , Michael P Pollastri 1 , Lori Ferrins 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-22 , DOI: 10.1021/acsmedchemlett.9b00455 Melissa J Buskes 1 , Monica Clements 1 , Kelly A Bachovchin 1 , Hitesh B Jalani 1 , Allison Leonard 1 , Seema Bag 1 , Dana M Klug 1 , Baljinder Singh 1 , Robert F Campbell 2 , Richard J Sciotti 2 , Nelly El-Sakkary 3 , Conor R Caffrey 3 , Michael P Pollastri 1 , Lori Ferrins 1
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We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
中文翻译：
拉帕替尼衍生类似物抗曼氏血吸虫的结构-生物活性关系
我们最近报道了一系列用于抗锥虫化合物溶解度驱动优化活动的化合物。将寄生虫跳跃方法扩展到该系列，对该库中的一部分化合物进行了交叉筛选，以确定其对抗后生扁虫寄生虫曼氏血吸虫的活性。这项研究报告了几种针对成虫血吸虫的有效生物活性化合物的鉴定和初步开发，其中一种或多种代表了进一步评估和优化的有希望的线索。
更新日期：2020-01-23
中文翻译：
拉帕替尼衍生类似物抗曼氏血吸虫的结构-生物活性关系
我们最近报道了一系列用于抗锥虫化合物溶解度驱动优化活动的化合物。将寄生虫跳跃方法扩展到该系列，对该库中的一部分化合物进行了交叉筛选，以确定其对抗后生扁虫寄生虫曼氏血吸虫的活性。这项研究报告了几种针对成虫血吸虫的有效生物活性化合物的鉴定和初步开发，其中一种或多种代表了进一步评估和优化的有希望的线索。
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