Electronic Resource
Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents
| العنوان: | Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents |
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| المؤلفون: | National Institute of Allergy and Infectious Diseases (US), Ministerio de Economía, Industria y Competitividad (España), Junta de Andalucía, Instituto de Salud Carlos III, Klug, Dana M. [0000-0002-8982-0640], Gamarro, Francisco [0000-0003-1347-3440], González-Pacanowska, D. [0000-0002-4303-5209], Navarro, M. [0000-0003-2301-2699], Pollastri, M.P. [0000-0001-9943-7197], Klug, Dana M., Díaz-González, Rosario, Pérez-Moreno, Guiomar, Ceballos-Pérez, Gloria, García-Hernández, Raquel, Gómez-Pérez, Veronica, Ruiz-Pérez, Luis Miguel, Rojas-Barros, Domingo I., Gamarro, Francisco, González-Pacanowska, Dolores, Martínez-Martínez, María S., Manzano, Pilar, Ferrins, Lori, Caffrey, Conor R., Navarro, M., Pollastri, M.P. |
| بيانات النشر: | Public Library of Science 2019-02-08 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | New treatments are needed for neglected tropical diseases (NTDs) such as Human African trypanosomiasis (HAT), Chagas disease, and schistosomiasis. Through a whole organism high-throughput screening campaign, we previously identified 797 human kinase inhibitors that grouped into 59 structural clusters and showed activity against T. brucei, the causative agent of HAT. We herein report the results of further investigation of one of these clusters consisting of substituted isatin derivatives, focusing on establishing structure-activity and -property relationship scope. We also describe their in vitro absorption, distribution, metabolism, and excretion (ADME) properties. For one isatin, NEU-4391, which offered the best activity-property profile, pharmacokinetic parameters were measured in mice. |
| مصطلحات الفهرس: | artículo |
| URL: | Publisher's version Sí MINECO/ICT2013-2016/SAF2015-71444-P MINECO/ICT2013-2016/SAF2016-79957-R |
| الاتاحة: | Open access content. Open access content https://creativecommons.org/licenses/by/4.0 openAccess |
| ملاحظة: | English |
| Other Numbers: | CTK oai:digital.csic.es:10261/178459 PLoS Neglected Tropical Diseases 1935-2727 10.1371/journal. pntd.0007129 1935-2735 1306014149 |
| المصدر المساهم: | CSIC From OAIster®, provided by the OCLC Cooperative. |
| رقم الانضمام: | edsoai.on1306014149 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |