8-Hydroxyquinolines with the potential for long-term anticaries activity: design, synthesis, and in vitro evaluation.
8-Hydroxyquinolyl benzoate and 8-hydroxyquinolyl para-(fluorosulfonyl)benzoate have been synthesized and evaluated in vitro as antimicrobial and antiplaque agents. Both compounds inhibited the growth of cultures of the following genera: Streptococcus, Staphylococcus, Actinomyces, Lactobacillus, Veillonella, and Candida. Minimum inhibitory concentrations ranged from 0.98 to 62 microgram/ml. Extracted human teeth pretreated with 1% solutions of either compound and rinsed with distilled water exhibited reduced in vitro plaque formation for 48 hours. These results indicate that the in vitro antiplaque activity of 8-hydroxyquinolines can be enhanced by attaching the appropriate side chain in the 8-position.
D001419:Bacteria / Q000187:drug effects; D001665:Binding Sites; D002327:Cariostatic Agents; D055598:Chemical Phenomena; D002621:Chemistry; D003692:Delayed-Action Preparations; D003773:Dental Plaque / Q000209:etiology / Q000517:prevention & control; D006801:Humans; D006912:Hydroxyquinolines / Q000494:pharmacology*; D015125:Oxyquinoline / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D013997:Time Factors; D014070:Tooth / Q000033:anatomy & histology
D002327:Cariostatic Agents; D003692:Delayed-Action Preparations; D006912:Hydroxyquinolines; D015125:Oxyquinoline