| Autor: |
Hongyi Zhao, Yongxin Gao, Wei Li, Li Sheng, Keli Cui, Bin Wang, Lei Fu, Meng Gao, Ziyun Lin, Xiaowen Zou, Mary Jackson, Haihong Huang, Yu Lu, Dongfeng Zhang |
| Rok vydání: |
2023 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 65(15) |
| ISSN: |
1520-4804 |
| Popis: |
In this work, pyrrole-2-carboxamides were designed with a structure-guided strategy based on the crystal structure of MmpL3 and a pharmacophore model. The structure-activity relationship studies revealed that attaching phenyl and pyridyl groups with electron-withdrawing substituents to the pyrrole ring and attaching bulky substituents to the carboxamide greatly improved anti-TB activity. Most compounds showed potent anti-TB activity (MIC0.016 μg/mL) and low cytotoxicity (IC |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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