Synthesis and in vitro evaluation of 8 hydroxyquinolines as dental plaque inhibitors

Article abstract of DOI:10.1002/jps.2600640934

Some 4 and 5 substituted 8 hydroxyquinolines, with predicted log P values in the range of 1.48 to 2.90, were synthesized by modified Skraup reactions or thermal cyclization. These hydroxyquinolines include the 5 methyl, 4,5 dimethyl, 4 methyl, 5 hydroxy 4 methyl, 5 methoxy, 5 methoxy 4 methyl, 4 hydroxy, 4 chloro, 4 amino, and 5 amino analogs. Partition coefficients, antibacterial activity, and antiplaque activity were determined. Four analogs showed in vitro antiplaque activity. None of the derivatives with ionizable functions was active.