8-Hydroxyquinolines with the potential for long-term anticaries activity: design, synthesis, and in vitro evaluation

J Dent Res. 1978 Jan;57(1):65-71. doi: 10.1177/00220345780570012401.

Abstract

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.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Bacteria / drug effects
  • Binding Sites
  • Cariostatic Agents*
  • Chemical Phenomena
  • Chemistry
  • Delayed-Action Preparations
  • Dental Plaque / etiology
  • Dental Plaque / prevention & control
  • Humans
  • Hydroxyquinolines / pharmacology*
  • Oxyquinoline / analogs & derivatives
  • Oxyquinoline / chemical synthesis
  • Oxyquinoline / pharmacology*
  • Time Factors
  • Tooth / anatomy & histology

Substances

  • Cariostatic Agents
  • Delayed-Action Preparations
  • Hydroxyquinolines
  • Oxyquinoline