RESUMEN
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.
Asunto(s)
Actinomyces/efectos de los fármacos , Aminopiridinas/farmacología , Antibacterianos , Placa Dental/microbiología , Streptococcus/efectos de los fármacos , Placa Dental/prevención & control , Humanos , Pruebas de Sensibilidad MicrobianaRESUMEN
A series of N,N'-polyalkylenebis[4-(substituted-amino)pyridines] has been prepared, and members have been evaluated as potential anti-dental plaque agents. From among the most active members of the series, one compound, N,N'-[1,10-decanediyldi-1(4H)-pyridinyl-4-ylidene]bis(1-octanam ine) dihydrochloride, octenidine, was selected as a candidate for clinical study.
Asunto(s)
Aminopiridinas/uso terapéutico , Placa Dental/tratamiento farmacológico , Humanos , Relación Estructura-ActividadAsunto(s)
Aceites Combustibles/provisión & distribución , Administración de Instituciones de Salud , Petróleo/provisión & distribución , Conservación de los Recursos Energéticos , Arquitectura y Construcción de Instituciones de Salud , Ambiente de Instituciones de Salud/organización & administración , Agencias de los Sistemas de Salud , Administración Hospitalaria , Servicio de Mantenimiento e Ingeniería en Hospital/organización & administración , Plásticos/provisión & distribución , Eliminación de Residuos , Estados UnidosRESUMEN
A series of bispyridines were examined for their bactericidal activities against in vitro, preformed, pure-culture plaques of selected oral plaque-forming bacteria. The antimicrobial activities of these agents were examined in relation to their molecular configurations. These studies demonstrated that the length of the interpyridine polymethylene group bridge and the length of the alkyl side chain were important determinants of antiplaque and antimicrobial efficacy. The most potent compounds of the bispyridine series were studied to determine the minimal conditions (concentration, duration, and frequency) of treatment required for likely clinical efficacy.