Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme and Mycobacterium tuberculosis
| Autor: | Pascal Hoffmann, Joëlle Azéma-Despeyroux, Fernanda Goncalves, Alessandro Stamilla, Nathalie Saffon-Merceron, Frédéric Rodriguez, Giulia Degiacomi, Maria Rosalia Pasca, Christian Lherbet |
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| Jazyk: | angličtina |
| Rok vydání: | 2024 |
| Předmět: | |
| Zdroj: | Molecules, Vol 29, Iss 13, p 3076 (2024) |
| Druh dokumentu: | article |
| ISSN: | 29133076 1420-3049 |
| DOI: | 10.3390/molecules29133076 |
| Popis: | Tuberculosis is a serious public health problem worldwide. The search for new antibiotics has become a priority, especially with the emergence of resistant strains. A new family of imidazoquinoline derivatives, structurally analogous to triazolophthalazines, which had previously shown good antituberculosis activity, were designed to inhibit InhA, an essential enzyme for Mycobacterium tuberculosis survival. Over twenty molecules were synthesized and the results showed modest inhibitory efficacy against the protein. Docking experiments were carried out to show how these molecules could interact with the protein’s substrate binding site. Disappointingly, unlike triazolophthlazines, these imidazoquinoline derivatives showed an absence of inhibition on mycobacterial growth. |
| Databáze: | Directory of Open Access Journals |
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