The in vitro dental plaque inhibitory properties of a series of N-[1-alkyl-4(1H)-pyridinylidene]alkylamines.
A series of novel N-[1-alkyl-4(1H)-pyridinylidene]alkylamine hydrohalides has been prepared and evaluated as inhibitors of dental plaque formation, in vitro. Several members of the series exhibited potency ca. 9-fold greater than that of chlorhexidine vs Streptococcus sobrinus 6715-13. The di-n-octyl analogue, 11 (pirtenidine), was found to be highly efficacious against several other oral plaque-forming microorganisms and is presently undergoing preclinical evaluation.
Wentland
M P
MP
Department of Medicinal Chemistry, Sterling-Winthrop Research Institute, Rensselaer, New York 12144.
Bailey
D M
DM
Powles
R G
RG
Slee
A M
AM
Sedlock
D M
DM
D000190:Actinomyces / Q000187:drug effects*; D000631:Aminopyridines / Q000494:pharmacology*; D000900:Anti-Bacterial Agents; D003773:Dental Plaque / Q000382:microbiology* / Q000517:prevention & control; D006801:Humans; D008826:Microbial Sensitivity Tests; D013291:Streptococcus / Q000187:drug effects*
D000631:Aminopyridines; D000900:Anti-Bacterial Agents