Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure–activity relationship studies
| Autor: | Salvatore Sanna Coccone, Luisa Chiasserini, Ettore Novellino, Maria Altarelli, Sandra Gemma, Caterina Camodeca, Stefania Butini, Giuseppe Campiani, Vinod Kumar, Giovanni Delogu, Luisa Savini, Pierangela Tripaldi, Sandra Clarizio |
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| Přispěvatelé: | Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Coccone, S. S., Kumar, V., Camodeca, C., Campiani, G., Novellino, Ettore, Clarizio, S., Delogu, G., Butini, S. |
| Rok vydání: | 2009 |
| Předmět: |
Tuberculosis
Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Chemical synthesis Settore MED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICA Cell Line Cercopithecus aethiops Mycobacterium tuberculosis Structure-Activity Relationship Chlorocebus aethiops Drug Discovery medicine Animals Structure–activity relationship Cytotoxicity Vero Cells Molecular Biology Antibacterial agent biology Chemistry Organic Chemistry Hydrazones biology.organism_classification medicine.disease In vitro Molecular Medicine Bacteria |
| Zdroj: | Bioorganic & Medicinal Chemistry. 17:6063-6072 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2009.06.051 |
| Popis: | A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25microg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results. |
| Databáze: | OpenAIRE |
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