4H-Pyran-4-one derivatives: leading molecule for preparation of compounds with antimycobacterial potential
4H-Pyran-4-one derivatives: leading molecule for preparation of compounds with antimycobacterial potential
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Tarih
2009-01-01
Yazarlar
Us, Demet
Gurdal, Ece
Berk, Barkin
Oktem, Sinem
Kocagoz, Tanil
Caglayan, Berrak
Kurnaz, Isil Aksan
Erol, Dilek Demir
Süreli Yayın başlığı
Süreli Yayın ISSN
Cilt Başlığı
Yayınevi
SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK
Dergi Adı
TURKISH JOURNAL OF CHEMISTRY
Özet
A series of 3-hydroxy-6-methyl-2-((4-substitutedpiperazin-1-yl)methyl)-4H-pyran-4-on e structured compounds were synthesized by reacting 5-hydroxy-2-methyl-4H-pyran-4-one with suitable piperazine derivatives using Mannich reaction conditions. Antibacterial activities of the compounds for E. coli, S. paratyphi, S. flexneri, E. gergoviae, and M. smegmatis were assessed in vitro by using broth dilution for determination of the minimum inhibitory concentration (MIC). In addition, their inhibitory effects over DNA gyrase enzyme were evaluated using a DNA gyrase supercoiling assay. Among the synthesized compounds
compound 7 showed a 4 mu g/mL MIC value for M. smegmatis, whereas the other compounds demonstrated moderate to high activity. Those tested in the supercoiling assay had at best a very mild inhibition of the enzyme. This series deserves further attention for testing over Mycobacterium species and topoisomerase II inhibition to develop new lead drugs.
compound 7 showed a 4 mu g/mL MIC value for M. smegmatis, whereas the other compounds demonstrated moderate to high activity. Those tested in the supercoiling assay had at best a very mild inhibition of the enzyme. This series deserves further attention for testing over Mycobacterium species and topoisomerase II inhibition to develop new lead drugs.
Açıklama
Anahtar kelimeler
Antimycobacterial activity, DNA gyrase activity, hydroxy-4H-pyran-4-one