Abstract:
:Periodontal disease is an oral chronic immune-inflammatory disease highly prevalent worldwide that is initiated by specific oral bacterial species leading to local and systemic effects. The development of new preventive/therapeutic strategies to specifically target oral periodontopathogens without perturbing oral microbiome species normally colonizing the oral cavity is needed. The fast and affordable strategy of repositioning of already FDA-approved drugs can be an answer to the development of novel treatments against periodontal pathogens such as Porphyromonas gingivalis. Herein, we report the synthesis and antibacterial activity of novel zafirlukast derivatives, their bactericidal effect, and their cytotoxicity against oral epithelial cell lines. Many of these derivatives exhibited superior antibacterial activity against P. gingivalis compared to the parent drug zafirlukast. The most promising compounds were found to be selective against P. gingivalis and they were bactericidal in their activity. Finally, we demonstrated that these potent derivatives of zafirlukast provided a better safety profile against oral epithelial cells compared to zafirlukast.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Thamban Chandrika N,Fosso MY,Alimova Y,May A,Gonzalez OA,Garneau-Tsodikova Sdoi
10.1039/c9md00074gsubject
Has Abstractpub_date
2019-06-10 00:00:00pages
926-933issue
6eissn
2040-2503issn
2040-2511pii
c9md00074gjournal_volume
10pub_type
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