ArticleAntimicrobial agents and chemotherapy2015
Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Anti-Mycobacterial Activity of Bacterial Topoisomerase Inhibitors with Dioxygenated Linkers.ACS infectious diseases · 2025Article
- Structural Aspects ofACS medicinal chemistry letters · 2024Article
- Molecular mechanism of a triazole-containing inhibitor ofiScience · 2024Article
- Interactions between Zoliflodacin andACS infectious diseases · 2024Article
- Gyrase and Topoisomerase IV: Recycling Old Targets for New Antibacterials to Combat Fluoroquinolone Resistance.ACS infectious diseases · 2024Review
- A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated byACS infectious diseases · 2023Article
- Article
- Why Matter Matters: Fast-TrackingMolecules (Basel, Switzerland) · 2022Review
- Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.Journal of medicinal chemistry · 2022Article
- Structure-Activity Relationship of Anti-ACS medicinal chemistry letters · 2022Article
- Identification of Antimycobacterial Natural Products from a Library of Marine Invertebrate Extracts.Medicines (Basel, Switzerland) · 2022Article
- "Upcycling" known molecules and targets for drug-resistant TB.Frontiers in cellular and infection microbiology · 2022Article
- A Mycobacterium tuberculosis NBTI DNA Gyrase Inhibitor Is Active against Mycobacterium abscessus.Antimicrobial agents and chemotherapy · 2021Article
- Resistance to Second-Line Anti-TB Drugs in Cambodia: A Phenotypic and Genetic Study.Infection and drug resistance · 2021Article
- A review of medicinal plant of Middle East and North Africa (MENA) region as source in tuberculosis drug discovery.Saudi journal of biological sciences · 2020Review
- Bimodal Actions of a Naphthyridone/Aminopiperidine-Based Antibacterial That Targets Gyrase and Topoisomerase IV.Biochemistry · 2019Article
- Impact of the host environment on the antitubercular action of pyrazinamide.EBioMedicine · 2019Review
- Article
- Mechanism of Action of Mycobacterium tuberculosis Gyrase Inhibitors: A Novel Class of Gyrase Poisons.ACS infectious diseases · 2018Article
- Inhibition of biofilm formation in Mycobacterium smegmatis by Parinari curatellifolia leaf extracts.BMC complementary and alternative medicine · 2017Article
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Authors and funding
16 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
One way to speed up the TB drug discovery process is to search for antitubercular activity among compound series that already possess some of the key properties needed in anti-infective drug discovery, such as whole-cell activity and oral absorption. Here, we present MGIs, a new series of Mycobacterium tuberculosis gyrase inhibitors, which stem from the long-term efforts GSK has dedicated to the discovery and development of novel bacterial topoisomerase inhibitors (NBTIs). The compounds identified were found to be devoid of fluoroquinolone (FQ) cross-resistance and seem to operate through a mechanism similar to that of the previously described NBTI GSK antibacterial drug candidate. The remarkable in vitro and in vivo antitubercular profiles showed by the hits has prompted us to further advance the MGI project to full lead optimization.
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