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Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-22 , DOI: 10.1021/acsmedchemlett.9b00453 Baljinder Singh 1 , Jean A Bernatchez 2 , Laura-Isobel McCall 2 , Claudia M Calvet 2 , Jasmin Ackermann 2 , Julia M Souza 2 , Diane Thomas 2 , Everton M Silva 2 , Kelly A Bachovchin 1 , Dana M Klug 1 , Hitesh B Jalani 1 , Seema Bag 1 , Melissa J Buskes 1 , Susan E Leed 3 , Norma E Roncal 3 , Erica C Penn 3 , Jessey Erath 4 , Ana Rodriguez 4 , Richard J Sciotti 3 , Robert F Campbell 3 , James McKerrow 2 , Jair L Siqueira-Neto 2 , Lori Ferrins 1 , Michael P Pollastri 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-22 , DOI: 10.1021/acsmedchemlett.9b00453 Baljinder Singh 1 , Jean A Bernatchez 2 , Laura-Isobel McCall 2 , Claudia M Calvet 2 , Jasmin Ackermann 2 , Julia M Souza 2 , Diane Thomas 2 , Everton M Silva 2 , Kelly A Bachovchin 1 , Dana M Klug 1 , Hitesh B Jalani 1 , Seema Bag 1 , Melissa J Buskes 1 , Susan E Leed 3 , Norma E Roncal 3 , Erica C Penn 3 , Jessey Erath 4 , Ana Rodriguez 4 , Richard J Sciotti 3 , Robert F Campbell 3 , James McKerrow 2 , Jair L Siqueira-Neto 2 , Lori Ferrins 1 , Michael P Pollastri 1
Affiliation
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Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
中文翻译：
支架和寄生虫跳跃：新的原生动物增殖抑制剂的发现
利用目标再利用和寄生虫跳跃方法，我们测试了先前报道的化合物库，这些化合物库对布氏锥虫具有活性，外加 31 种新化合物，可对抗各种原生动物寄生虫，包括克氏锥虫、主要利什曼原虫、多诺瓦尼利什曼原虫和恶性疟原虫。这导致发现了几种具有亚微摩尔活性和改善物理化学性质的化合物，这些化合物是开发针对动质体疾病和疟疾的化学治疗剂的早期线索。
更新日期：2020-01-23
中文翻译：
支架和寄生虫跳跃：新的原生动物增殖抑制剂的发现
利用目标再利用和寄生虫跳跃方法，我们测试了先前报道的化合物库，这些化合物库对布氏锥虫具有活性，外加 31 种新化合物，可对抗各种原生动物寄生虫，包括克氏锥虫、主要利什曼原虫、多诺瓦尼利什曼原虫和恶性疟原虫。这导致发现了几种具有亚微摩尔活性和改善物理化学性质的化合物，这些化合物是开发针对动质体疾病和疟疾的化学治疗剂的早期线索。
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