دورية أكاديمية
Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme and Mycobacterium tuberculosis
العنوان: | Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme and Mycobacterium tuberculosis |
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المؤلفون: | Pascal Hoffmann, Joëlle Azéma-Despeyroux, Fernanda Goncalves, Alessandro Stamilla, Nathalie Saffon-Merceron, Frédéric Rodriguez, Giulia Degiacomi, Maria Rosalia Pasca, Christian Lherbet |
المصدر: | Molecules, Vol 29, Iss 13, p 3076 (2024) |
بيانات النشر: | MDPI AG, 2024. |
سنة النشر: | 2024 |
المجموعة: | LCC:Organic chemistry |
مصطلحات موضوعية: | mycobacterium tuberculosis, InhA enzyme, inhibitor, imidazoquinoline, triazolophthalazine, Organic chemistry, QD241-441 |
الوصف: | 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. |
نوع الوثيقة: | article |
وصف الملف: | electronic resource |
اللغة: | English |
تدمد: | 29133076 1420-3049 |
Relation: | https://www.mdpi.com/1420-3049/29/13/3076; https://doaj.org/toc/1420-3049 |
DOI: | 10.3390/molecules29133076 |
URL الوصول: | https://doaj.org/article/2c1ad0e2eed648a4ab889c946f63fcb2 |
رقم الأكسشن: | edsdoj.2c1ad0e2eed648a4ab889c946f63fcb2 |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 29133076 14203049 |
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DOI: | 10.3390/molecules29133076 |