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KMID : 0370019870010000056
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Chung-Ang Journal of Pharmacal Sciences
1987 Volume.1 No. 0 p.56 ~ p.68
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Studies on the syntheses of Aliphatic Alkylene Bisthiourea Derivatives and their Antimic robial Activities
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이현수/Lee, Hyun, Soo
임철부/Yim, Chul Bu
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Abstract
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The eighteen new aliphatic alklene bisthiourea derivatives were synthesized and evaluated for antimicrobial activities. Treatment of aliphatic amines with carbondisulfide, sodium hydroxide and ethylchlorofomate provided alkylisothiocyanates. Reaction of alkyl isothiocyanates with alkylenediamines yielded α, ω-bis (N^3-alkyl-N^1-thioureido) alkanes.
The compounds synthesized were subjected in vitro for antimicrobial activities against Mycobacterium phlei, Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, and Escherichia coli.
The results obtained were as follows :
1) 1,4-bis(N^3-n-butyl-N^1-thjoureido) butane(18) showed the growth inhibitory activities against Mycobacterium phlei at the concentration of 0.25㎍ / ml, and against Bacillus subtilis at 15.63㎍ / ml.
2) 1,4-bis(N^3-isobutyl-N^1-thioureido) butane(17) exhibited the growth inhibitory activity against Mycobacterium phlei at the concentration of 0.49 ㎍ / ml.
3) 1,2-bis(N^3-isobutyl-N^1-thioureido) ethane(11) exhibited the growth inhibitory activity against Staphylococcus epidermidis at the concentration of 7.8㎍ / ml.
4) In general, tetramethylene bisthiourea derivatives showed potent antimicrobial activities against Mycobacterium phlei
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