著者
野口 照久 橋本 喜信 小坂 璋吾 菊池 正義 宮崎 幸信 先本 礼次 加治 有恒
出版者
公益社団法人 日本薬学会
雑誌
YAKUGAKU ZASSHI (ISSN:00316903)
巻号頁・発行日
vol.88, no.3, pp.344-352, 1968-03-25 (Released:2008-05-30)
参考文献数
21

Some observations were made on the anti-trichophyton action of 2-naphthyl N-methyl-N-arylthiocarbamate (A). In vitro antifungal activity decreased slightly when the thiocarbamate was changed to carbamate, and a marked lowering in the in vitro effect was observed. The antifungal activity disappeared entirely when the thiocarbamate was changed to dithiocarbamate and thiolcarbamate. When the aryl group in A is a naphthyl, antifungal activity is present only when 1-naphthyl is present and other three combinations are entirely ineffective. When the aryl is a substituted phenyl, compounds having methyl, methoxyl, or halogens, those with the Hammet constant in the range of +0.23 to -0.27, have marked antitrichophyton activity in vivo, but those with nitro, formyl, carboxyl, sulfonamido hydroxyl, or dimethylamino group show marked decrease in the effect. The series of compounds having the A type will henceforth be designated as naphthiomates.
著者
野口 照久 小坂 璋吾 橋本 喜信 菊池 正義 宮崎 幸信 加治 有恒
出版者
公益社団法人 日本薬学会
雑誌
YAKUGAKU ZASSHI (ISSN:00316903)
巻号頁・発行日
vol.88, no.3, pp.353-358, 1968-03-25 (Released:2008-05-30)
参考文献数
16
被引用文献数
1 2

Examinations were made on the effect of oral administration of 2-naphthyl N-methyl-N-arylthiocarbamates (naphthiomates), an effective antimicotic agent for external use, against experimental trichophytosis. Finely powdered 2-naphthyl N-methyl-N-(m-tolyl)-thiocarbamate (naphthiomate-T) and 2-naphthyl N-methyl-N-(1-naphthyl) thiocarbamate (naphthiomate-N) showed an effect comparable to griseofulvin in about four-fold dose of the latter. In vivo metabolism of naphthiomate-T was examined in guinea pigs and rabbits, and it was found that the majority is excreted in the feces without decomposition, and little is absorbed through the intestinal tract. N-Methyl-m-toluidine and β-naphthol were detected from urine, feces, and blood as the metabolites.