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Inability of Isoquinoline Derivatives to Inhibit Virus Neuraminidase Activity

Central Research Laboratories, Sankyo Co., Ltd, 2-58 1-chome Hiromachi Shinagawa-ku Tokyo Japan

The antivirus activity of isoquinoline derivatives, 1-(p-chlorophenoxymethyl)-3, 4-dihydroisoquinoline hydrochloride (compound I) and 1-(p-methoxyphenoxymethyl)-3, 4-dihydroisoquinoline hydrochloride (compound II) has been demonstrated by many studies in vitro and in vivo on several agents of human respiratory diseases. The mechanism by which these compounds inhibit the multiplication of influenza viruses was presumed to be due to their antineuraminidase activity (Tute et al. 1970).

During an investigation on the antivirus effect of isoquinoline derivatives, we found that both derivatives did not inhibit the enzyme reaction but blocked only the colour development of N-acetylneuraminic acid (NANA). This brief report will be concerned with the results obtained regarding this problem.

Influenza virus A₂/JAPAN-305 (Chiba), partially purified from infected chorioallantoic fluid, was used as a virus enzyme source. The enzyme activity was measured by a slight modification of the method described by Rafelson, Gold, & Priede (1966).

Received 24 February 1972; accepted 3 May 1972.