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KMID : 0370019870010000106
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Chung-Ang Journal of Pharmacal Sciences
1987 Volume.1 No. 0 p.106 ~ p.117
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The studies on the syntheses of aromatic alkylene bisthio urea derivatives and their antimicrobial activities
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조영수/Cho Young Soo
임철부/Yim Chul Bu
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Abstract
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The eighteen new aromatic alkylene bisthiourea derivatives were synthesized and evaluated for antimicrobial activities. Treatment of aromatic amines with carbondisulfide, ammonia and lead nitrate provided arylisothiocyanates. Reaction of arylisothiocyanates with ethylenediamine yielded 1,2-bis(N^3-aryl-N^3-thioureido) ethanes. 1,4-bis(N^3-aryl-N^1-thioureido) butanes were obtained by the reaction fo 1,4-diaminobutane with arylisothiocyanates. 1,6-bis(N^3-aryl-N^1-thioureido) hexanes were also prepared by treating 1,6-diaminohexane with arylisothiocyanates. The compounds synthesized were subjected in vitro for antimicrobial activities against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichea coli, and Mycobacterium phlei. The most active compound, 1,2-bis-(N^3-p-chloropheny-N^1-thioureido)ethane (1), showed the growth inhibitory activity against Mycobacterium phlei and Staphylococcus aureus at 7.82 ㎍ / ml. 1,2-bis(N^3-p-bromophenyl-N^1-thioureido) ethane(4) exhibited the growth in hibitory activity against Mycobacterium phlei at the concentration of 1.96㎍ / ml. In general, the compounds synthesized were showed potent antimicrobial activity against Mycobacterium phlei.
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