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KMID : 0370019910050000075
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Chung-Ang Journal of Pharmacal Sciences
1991 Volume.5 No. 0 p.75 ~ p.86
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Syntheses of Alkylthiocarbamylpiperazine Derivatives and Their Antimicrobial Activities
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Abstract
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The twelve new alkylthiocarbamylpiperazine derivatives and six alkythiocarbamylmorpholine derivatives were synthesized and evaluated for their antimicrobial activities.
1,4-Bis(N-alkythiocarbamyl) piperazines were prepared by treating piperazine with alkylisothiocyanates, which were obtained by the reaction of alkylamines with carbondisulfide, sodiumhydroxide, ethyl chloroformate.
The treatment of 1-methylpiperazine with alkylisothiocyanates yielded 1-methyl-4-(N-alkylthiocarbamyl) piperazines.
4(N-alkylthiocarbamyl) morpholines were also synthesized by the reaction of morpholine with alkylisothiocyanates.
Antimicrobial activities of the synthesized compounds were examined in vitro against Mycobacterium phloei, Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis and Escherichia coli.
The results obtained were as follow :
The most active compounds(XX, XXⅡ, XXⅢ, XXⅥ) showed the growth inhibitory activity against S. aureus at the concentration of 7.82㎍/㎖.
1,4-Bis(N-n-propylthiocarbamyl) piperazine(X) and 1,4-Bis(N-n-butylthiocarbamyl) piperazine(XⅡ) showed the growth inhibitory activity against B. subtilis at the concetration of 31.25㎍/㎖, respectively.
1-Methyl-4(N-n-butylthiocarbamyl) piperazine(XⅧ) exhibited the growth inhibitory activity against M. phlei at the concentration of 15.63㎍/㎖.
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