YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Studies on Chemotherapeutic Agents Against Mycobacterium Tuberculosis. XXVI. : Synthesis and Antituberculous Activity of Phenylthiourea, p-Ethoxyphenylthiourea and 3-Bromo-4-ethoxyphenylthiourea Derivatives
FUKUJIRO FUJIKAWA, KUNIO HIRAI, TERUHISA HIRAYAMA, TERUKI MATSUNASHI, YOSHIKUNI NAKANISHI, KAYOKO KUMOTO, TATSUZO SHIMIZU, CHIICHIRO SAKAKI, YOSHITARO HAMURO, MITSUNORI IKEDA, YASUHIKO MICHISHITA, YOKO ISHITOMI, MASUKAZU NAITO, NOBUO MAEKAWA, SHUNJI TSUKUMA, MITSURU KAWAI
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1971 Volume 91 Issue 2 Pages 159-165

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Abstract
A total of 75 kinds of compounds, comprising 27 kinds of phenylthiourea derivatives, 25 kinds of p-ethoxyphenylthiourea derivatives, and 23 kinds of 3-bromo-4-ethoxyphenylthiourea derivatives, were synthesized and screened for antibacterial activity using sensitive strain of human-type tubercle bacilli H37Rv with Tween-albumin medium, by the in vitro multiple dilution method. Inhibition of bacillary growth by the control agents was found in 0.0313 μg/ml of INH, 0.08-0.156 μg/ml of TBI, 0.313 μg/ml of PAS, and 1.56-3.13 μg/ml of DAT, but none of the synthesized compounds showed better activity, growth inhibition being seen with 3.13 μg/ml of 1-phenyl-3-(4-dimethylaminophenyl)-2-thiourea and with 6.25 μg/ml of 1-phenyl-3-(2-ethylhexyl)-, 1-(4-ethoxyphenyl)-3-(4-bromophenyl)-, 1-(4-ethoxyphenyl)-3-(4-acetylphenyl)-, 1-(4-ethoxyphenyl)-3-(4-butoxycarbonylphenyl)-, and 1-(4-ethoxyphenyl)-3-(2-diphenyl)-2-thioureas.
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