Oxadiazoles Have Butyrate-Specific Conditional Activity against Mycobacterium tuberculosis
| Autor: | Mai A. Bailey, Maria Angeles Martinez-Grau, Yulia Ovechkina, Allen Casey, Tanya Parish, Isabel C. Gonzalez Valcarcel, Torey Alling, Juliane Ollinger, Michal Vieth, Megan Files, Julie V. Early |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Tuberculosis Cell Survival Phenotypic screening 030106 microbiology Antitubercular Agents Oxadiazole Levofloxacin Microbial Sensitivity Tests Butyrate Biology Microbiology Small Molecule Libraries Mycobacterium tuberculosis Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Species Specificity Kanamycin Chlorocebus aethiops Isoniazid medicine Animals Experimental Therapeutics Pharmacology (medical) Cytotoxicity Vero Cells Pathogen Pharmacology Oxadiazoles biology.organism_classification medicine.disease Culture Media High-Throughput Screening Assays Glucose 030104 developmental biology Infectious Diseases chemistry Butyric Acid Specific activity Metabolic Networks and Pathways |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 60:3608-3616 |
| ISSN: | 1098-6596 0066-4804 |
| Popis: | Mycobacterium tuberculosis is a global pathogen of huge importance which can adapt to several host niche environments in which carbon source availability is likely to vary. We developed and ran a phenotypic screen using butyrate as the sole carbon source to be more reflective of the host lung environment. We screened a library of ∼87,000 small compounds and identified compounds which demonstrated good antitubercular activity against M. tuberculosis grown with butyrate but not with glucose as the carbon source. Among the hits, we identified an oxadiazole series (six compounds) which had specific activity against M. tuberculosis but which lacked cytotoxicity against mammalian cells. |
| Databáze: | OpenAIRE |
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