Journal of Pharmaceutical Sciences p. 1563 - 1566 (1975)
Update date:2022-08-25
Topics:
Warner
Musto
Turesky
Soloway
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.
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