Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines
| Autor: | Morten Brændvang, Matthew Lovell Read, Pedro O. Miranda, Lise-Lotte Gundersen |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
medicine.drug_class Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Antimycobacterial Biochemistry Chemical synthesis Mycobacterium tuberculosis Pyrimidine analogue Structure-Activity Relationship Drug Discovery medicine Purine metabolism Molecular Biology Antibacterial agent biology Chemistry Organic Chemistry Biological activity biology.organism_classification Anti-Bacterial Agents Pyrimidines Purines Molecular Medicine Antibacterial activity |
| Zdroj: | Bioorganicmedicinal chemistry. 18(11) |
| ISSN: | 1464-3391 |
| Popis: | Pyrimidine analogs of antimycobacterial 6-aryl-9-benzylpurines have been synthesized and screened for antibacterial activity against Mycobacterium tuberculosis H 37 Rv in vitro. Several active compounds were identified and the best results were observed for 5-formamidopyrimidines. These compounds generally displayed IC 90 values ≤1 μg/mL, and they exhibited low toxicity towards mammalian cells. Imidazolylpyrimidines, which may be regarded as fleximer analogs of the parent purines, were also synthesized and one of them was found to be quite a potent inhibitor of M. tuberculosis (IC 90 14 μg/mL). |
| Databáze: | OpenAIRE |
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