Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives. Bioorganic & medicinal chemistry. [Bioorg Med Chem] Journal article | | Title | Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives. | | Author(s) | Zarranz B, Jaso A, Aldana I, Monge A | | Institution | Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, Pamplona, Spain. | | Source | Bioorg Med Chem 2003 May 15; 11(10):2149-56. | | MeSH | Animals
Antitubercular Agents
Cell Survival
Cercopithecus aethiops
Macrophages
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis
Nitriles
Quinoxalines
Structure-Activity Relationship
Vero Cells
| | Abstract | As a continuation of our research and with the aim of obtaining new antituberculosis agents which can improve the current chemotherapeutic antituberculosis treatments, new series of quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis strain H(37)Rv, using the radiometric BACTEC 460-TB methodology. Active compounds were also screened by serial dilution to assess toxicity to a VERO cell line. The results indicate that some compounds exhibited a good antituberculosis activity and the arylcarboxamide analogues 3, 8, and 9 were the most active compounds (EC(90)/MIC1). Also, the cytotoxic effects indicate that these compounds have a good Selectivity Index (SI). | | Language | eng | | Pub Type(s) | Journal Article
| | PubMed ID | 12713824 |
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