In vitro and in vivo Activity of K-130, a Dihydrofolate Reductase inhibitor, against Mycobacterium leprae
| Autor: | Dhople Am |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Leprostatic Agents
Microbial Sensitivity Tests Dapsone Microbiology Mice Minimum inhibitory concentration In vivo Drug Discovery Dihydrofolate reductase medicine Animals Sulfones Mycobacterium leprae Antibacterial agent Mice Inbred BALB C biology Foot Drug Resistance Microbial Drug Synergism biology.organism_classification Dihydrofolate reductase inhibitor In vitro Pyrimidines biology.protein Folic Acid Antagonists Female medicine.drug |
| Zdroj: | Arzneimittelforschung. 49:267-271 |
| ISSN: | 1616-7066 0004-4172 |
| DOI: | 10.1055/s-0031-1300412 |
| Popis: | The antimicrobial effects of a new dihydrofolate reductase inhibitor, K-130 (2,4-diaminodiphenyl sulfone substituted 2,4-diamino-5-benzylpyrimidine), alone and in combination with dapsone (CAS 80-08-0) against both dapsone-sensitive and dapsone-resistant strains of Mycobacterium leprae were evaluated in vitro, in cell-free culture system, and in vivo, in mouse foot pads. The minimal inhibitory concentration of K-130 against dapsone-sensitive as well as dapsone resistant strains of M, leprae was 0.03 microgram/ml, and the activity was bactericidal in both cases. However, when combined with dapsone, K-130 exhibited synergism in case of dapsone-sensitive M. leprae, while in case of dapsone-resistant M. leprae, the effect was merely additive. Similar synergistic effects were also observed in the mouse foot pad system for both types of M. leprae strains. |
| Databáze: | OpenAIRE |
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