Selective anti-tubercular purines: Synthesis and chemotherapeutic properties of 6-aryl- and 6-heteroaryl-9-benzylpurines
| Autor: | Morten Brændvang, Lise-Lotte Gundersen |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Purine
Staphylococcus aureus Stereochemistry Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Antineoplastic Agents Biochemistry Chemical synthesis Cell Line Mycobacterium tuberculosis Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Chlorocebus aethiops Drug Discovery Escherichia coli Animals Cytotoxicity Purine metabolism Vero Cells Molecular Biology Cell Proliferation Antibacterial agent Molecular Structure biology Aryl Organic Chemistry biology.organism_classification chemistry Purines Molecular Medicine Bacteria |
| Zdroj: | Bioorganic & Medicinal Chemistry. 13:6360-6373 |
| ISSN: | 0968-0896 |
| Popis: | 6-Aryl- and 6-heteroaryl-9-benzylpurines have been synthesized employing palladium-catalyzed coupling reactions in the step forming the C-C or C-N bond between the aryl- or heteroaryl and the purine. The compounds were screened for activity against Mycobacterium tuberculosis as well as representative Gram+ and Gram- bacteria, and for cytotoxic effects on mammalian cells. Several potent antimycobacterials were identified. These compounds probably act by a novel and selective mechanism; they exhibit low toxicity toward other bacteria as well as mammalian cells. |
| Databáze: | OpenAIRE |
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