1. An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
- Author
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Kaushik A, Heuer AM, Bell DT, Culhane JC, Ebner DC, Parrish N, Ippoliti JT, and Lamichhane G
- Subjects
- Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Dose-Response Relationship, Drug, Gram-Negative Bacteria drug effects, Gram-Negative Bacteria growth & development, Gram-Positive Bacteria growth & development, Microbial Sensitivity Tests, Molecular Structure, Oxazolidinones chemical synthesis, Oxazolidinones chemistry, Structure-Activity Relationship, Anti-Bacterial Agents pharmacology, Gram-Positive Bacteria drug effects, Oxazolidinones pharmacology
- Abstract
Innovation of new antibacterials that are effective against strains that have developed resistance to existing drugs would strengthen our ability to treat and subsequently control spread of pathogenic bacteria. Increasing incidence of infections with drug resistant bacteria has become a common occurrence in recent times. We have developed an evolved oxazolidinone, T145, which inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. The oxazolidinone is bactericidal against Mtb but bacteriostatic against E. faecalis and S. aureus. In addition to therapeutically valuable potency and bactericidal activity against Mtb, T145 minimizes selection of spontaneous resistant mutants, a trait that prolongs longevity of a drug in clinical use., (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Published
- 2016
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