Structure-activity relationship studies on niphimycin, a guanidylpolyol macrolide antibiotic. Part 1: The role of the N-methyl-N'-alkylguanidinium moiety |
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Authors: | Usuki Yoshinosuke Matsumoto Keiji Inoue Takatsugu Yoshioka Koichi Iio Hideo Tanaka Toshio |
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Affiliation: | Department of Material Science, Graduate School of Science, Osaka City University, 3-3-138 Sugimoto, Sumiyoshi-ku, Osaka 558-8585, Japan. usuki@sci.osaka-cu.ac.jp |
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Abstract: | Several N-methyl-N'-alkylguanidinium derivatives were synthesized and used as simplified analogues of niphimycin (NM), a guanidylpolyol macrolide, in structure-activity relationship studies. The C16-alkylated derivative exerted fungicidal activity by directly damaging the fungal plasma membrane and inducing oxidative stress in a manner similar to niphimycin. These results indicate that the N-methyl-N'-alkylguanidinium moiety is required for antifungal activity by NM. |
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