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Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-Oxide derivatives
- Source :
- Bioorganic & Medicinal Chemistry. 11:2149-2156
- Publication Year :
- 2003
- Publisher :
- Elsevier BV, 2003.
-
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).
- Subjects :
- Serial dilution
Cell Survival
medicine.drug_class
Stereochemistry
Clinical Biochemistry
Antitubercular Agents
Pharmaceutical Science
Carboxamide
Microbial Sensitivity Tests
Antimycobacterial
Biochemistry
Chemical synthesis
Mycobacterium tuberculosis
Structure-Activity Relationship
chemistry.chemical_compound
Quinoxaline
Quinoxalines
Chlorocebus aethiops
Nitriles
Drug Discovery
medicine
Animals
Structure–activity relationship
Vero Cells
Molecular Biology
Antibacterial agent
Molecular Structure
biology
Macrophages
Organic Chemistry
biology.organism_classification
chemistry
Molecular Medicine
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....82d7291347cbc989e28c8ac443b1674e