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KMID : 0370019960100000231
Chung-Ang Journal of Pharmacal Sciences
1996 Volume.10 No. 0 p.231 ~ p.236
Antimicrobial Activity of Benzothiazolyl Biguanides



Abstract
The twenty benzothiazolyl biguanides synthesized were evaluated for their antimicrobial activities against Staphylococcus aureus. Bacillus subtilis, Mycobacterium phlei, Escherichia coli, Microsporium canis, Candida albicans, Sporothrix schenkii and Trichophyton mentagrophytes. The results obtained were as follow : The most active compound, 1,6-bis£ûN^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido£ý hexane¡¤2HCI (14) showed the growth inhibitory activity against S. aureus at the concentration of 7.81ug/mL, against B.subtilis at 15.63ug/mL and against M. phlei at 31.25ug/mL. 1,6-Bis £ûN^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido£ý hexane¡¤2HCI(14), 1,6-Bis£ûN^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido) hexane¡¤2HCI (15) and N-(6-chlorobenzothiazol-2-yl)-1-piperidinylamidinoamidine¡¤HCI (24) inhibited the growth of M. phlei at the concentration of 31.25ug/mL respectively. 1,4-Bis£ûN^5-(6-methylbenzothiazol-2yl)-N^1-biguanido£ýbutane¡¤2HCI(9) and 1,4-bis£ûN^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido£ýbutane¡¤2HCI(11) exhibited the antimicrobial activity against B.subtilils at the concentration of 31.25ug/mL. Twelve new biguanide compounds showed growth inhibitory activities against C. albicans at the concentration of 400ug/mL.
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