دورية أكاديمية
Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening
| العنوان: | Novel chemical entities inhibiting Mycobacterium tuberculosis growth identified by phenotypic high-throughput screening |
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| المؤلفون: | Anuradha Kumar, Somsundaram Chettiar, Brian S. Brown, Julie Early, Juliane Ollinger, Megan Files, Mai A. Bailey, Aaron Korkegian, Devon Dennison, Matthew McNeil, James Metz, Augustine Osuma, Michael Curtin, Aaron Kunzer, Gail Freiberg, Milan Bruncko, Dale Kempf, Tanya Parish |
| المصدر: | Scientific Reports, Vol 12, Iss 1, Pp 1-27 (2022) |
| بيانات النشر: | Nature Portfolio, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Medicine LCC:Science |
| مصطلحات موضوعية: | Medicine, Science |
| الوصف: | Abstract We performed a high-throughput phenotypic whole cell screen of Mycobacterium tuberculosis against a diverse chemical library of approximately 100,000 compounds from the AbbVie corporate collection and identified 24 chemotypes with anti-tubercular activity. We selected two series for further exploration and conducted structure–activity relationship studies with new analogs for the 4-phenyl piperidines (4PP) and phenylcyclobutane carboxamides (PCB). Strains with mutations in MmpL3 demonstrated resistance to both compound series. We isolated resistant mutants for the two series and found mutations in MmpL3. These data suggest that MmpL3 is the target, or mechanism of resistance for both series. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2045-2322 |
| Relation: | https://doaj.org/toc/2045-2322 |
| DOI: | 10.1038/s41598-022-19192-7 |
| URL الوصول: | https://doaj.org/article/a7bda231d18f419a8fd60f4ebad065f6 |
| رقم الأكسشن: | edsdoj.7bda231d18f419a8fd60f4ebad065f6 |
| قاعدة البيانات: | Directory of Open Access Journals |
Find this article in full text from Springer Verlag. 
Full Text Finder | تدمد: | 20452322 |
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| DOI: | 10.1038/s41598-022-19192-7 |