ArticleAntimicrobial agents and chemotherapy1993
In vitro and in vivo activities of the nitroimidazole CGI 17341 against Mycobacterium tuberculosis.
Article in Antimicrobial agents and chemotherapy, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed.
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- Insights into anti-tuberculosis drug design on the scaffold of nitroimidazole derivatives using structure-based computer-aided approaches.RSC advances · 2025Article
- Recent Biochemical Advances in Antitubercular Drugs: Challenges and Future.Current topics in medicinal chemistry · 2024Review
- Discovery and characterization of antimycobacterial nitro-containing compounds with distinct mechanisms of action andAntimicrobial agents and chemotherapy · 2023Article
- SigH stress response mediates killing of Mycobacterium tuberculosis by activating nitronaphthofuran prodrugs via induction of Mrx2 expression.Nucleic acids research · 2023Article
- Advances of new drugs bedaquiline and delamanid in the treatment of multi-drug resistant tuberculosis in children.Frontiers in cellular and infection microbiology · 2023Review
- Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950-2021 Comprehensive Overview.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Delamanid or pretomanid? A Solomonic judgement!The Journal of antimicrobial chemotherapy · 2022Article
- Cofactor F420: an expanded view of its distribution, biosynthesis and roles in bacteria and archaea.FEMS microbiology reviews · 2021Article
- Synthesis of imidazo-1,4-oxazinone derivatives and investigation of reaction mechanism.Turkish journal of chemistry · 2021Article
- Recent Progress in the Discovery and Development of 2-Nitroimidazooxazines and 6-Nitroimidazooxazoles to Treat Tuberculosis and Neglected Tropical Diseases.Molecules (Basel, Switzerland) · 2020Review
- Molecule Property Analyses of Active Compounds forJournal of medicinal chemistry · 2020Review
- Antitubercular Triazines: Optimization and Intrabacterial Metabolism.Cell chemical biology · 2020Article
- High-Content Screening of Eukaryotic Kinase Inhibitors Identify CHK2 Inhibitor Activity AgainstFrontiers in microbiology · 2020Article
- Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.Journal of medicinal chemistry · 2018Article
- Multidirectional Efficacy of Biologically Active Nitro Compounds Included in Medicines.Pharmaceuticals (Basel, Switzerland) · 2018Review
- Challenging the Drug-Likeness Dogma for New Drug Discovery in Tuberculosis.Frontiers in microbiology · 2018Review
- Synthesis and Utilization of Nitroalkyne Equivalents in Batch and Continuous Flow.Angewandte Chemie (International ed. in English) · 2017Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CGI 17341 (2-ethyl-5-nitro-2,3-dihydro[2-1b]imidazo-oxazole) is a novel orally active representative of the 5-nitroimidazole series of antimicrobial agents. At concentrations ranging from 0.1 to 0.3 micrograms/ml, CGI 17341 inhibited the drug-susceptible and multi-drug-resistant strains of Mycobacterium tuberculosis. CGI 17341 had no cross-resistance with isoniazid, rifampin, streptomycin, or ethambutol. While the in vitro activity of CGI 17341 against M. tuberculosis was comparable to those of isoniazid and rifampin, it was superior to those of streptomycin, ciprofloxacin or norfloxacin, and oxazolidinone DuP 721. The MIC of CGI 17341 was not affected when the pH of the medium was decreased from 6.8 to 5.6, while four- to sixfold increases in the MICs of ciprofloxacin and isoniazid were observed. In mice infected with M. tuberculosis, the 50% effective dose for CGI 17341 was 7.7 mg/kg of body weight (95% confidence limits, 3.5 and 10.27) when administered on days 11 and 12 postinfection. CGI 17341 gave a dose-dependent (r = 0.995) and significant increase in the survival time. Our data indicate that the 5-nitroimidazole CGI 17341 is a promising and novel antituberculosis compound with potent in vitro and in vivo activities. Further investigations on this compound are warranted.
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