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Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme and Mycobacterium tuberculosis

التفاصيل البيبلوغرافية
العنوان: Imidazoquinoline Derivatives as Potential Inhibitors of InhA Enzyme and Mycobacterium tuberculosis
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
الوصف
تدمد:29133076
14203049
DOI:10.3390/molecules29133076