| Autor: |
Renata Jardim Etchart, Raoní S. Rambo, Bruno Lopes Abbadi, Nathalia Sperotto, Christiano Ev Neves, Fernanda Fries Silva, Maiele Dornelles, Lovaine Duarte, Fernanda Souza Macchi, Marcia Alberton Perelló, Rogério Vescia Lourega, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado |
| Jazyk: |
angličtina |
| Rok vydání: |
2021 |
| Předmět: |
|
| Zdroj: |
Molecules, Vol 26, Iss 17, p 5148 (2021) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/molecules26175148 |
| Popis: |
Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20 1H-indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Furthermore, the top hit compounds were active against multidrug-resistant strains, without cross-resistance with first-line drugs. Exposing HepG2 and Vero cells to the molecules for 72 h showed that one of the evaluated structures was devoid of apparent toxicity. In addition, this 3-phenyl-1H-indole showed no genotoxicity signals. Finally, time-kill and pharmacodynamic model analyses demonstrated that this compound has bactericidal activity at concentrations close to the Minimum Inhibitory Concentration, coupled with a strong time-dependent behavior. To the best of our knowledge, this study describes the activity of 3-phenyl-1H-indole against Mtb for the first time. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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