As part of a general investigation of new antibacterial agents,1 we have prepared a series of 1-alkyl-1,8-naphthyridin-4-one-3-carboxylic acid derivatives. Several members of the series, listed in Table I, were found to be highly effective antibacterial agents both in vitro and in vivo.These 1-alkyl-1,8-naphthyridines are prepared as outlined. The appropriate 6-substituted-2-aminopyridine (I) is condensed with diethyl ethoxymethylenemalonate and the resulting diethyl N-(6substituted-2-pyridyl)-aminomethylenemalonate (II) is cyclized in refluxing Dowtherm A or diethyl phthalate to give the ethyl 4-hydroxy-1,8-naphthyridine-3-carboxylate derivative (III).2 Hydrolysis of the ester (III) to the corresponding acid and alkylation in alcoholwater with potassium hydroxide gives the desired 1-alkyl-1,8-naphthyridin-4-one-3-carboxylic acid (IV). Alternatively, the same
Benzalkonium chloride (as Roccal or Zephiran) was found to inactivate influenza, measles, canine distemper, rabies, fowl laryngotracheitis, vaccinia, Semliki Forest, feline pneumonitis, meningopneumonitis, and herpes simplex viruses after 10 min of exposure at 30 C or at room temperature. Poliovirus and encephalomyocarditis virus were not inactivated under the same conditions. It was concluded that all viruses tested were sensitive except members of the picorna group. The literature was reviewed.
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