Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 1 |
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| Authors: | Masubuchi K Okada T Kohchi M Sakaitani M Mizuguchi E Shirai H Aoki M Watanabe T Kondoh O Yamazaki T Satoh Y Kobayashi K Inoue T Horii I Shimma N |
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| Institution: | Department of Chemistry, Nippon Roche Research Center, Kanagawa, Japan. |
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| Abstract: | Highly potent 1,3-beta-D-glucan synthase inhibitors 10, 11 and 13 have been identified by the chemical modification of the fungicidal macrocyclic lipopeptidolactone, RO-09-3655 (1), isolated from the cultured broth of Deuteromycotinia spp. D-Ornithine derivative (10) showed improved antifungal activity in the systemic candidiasis model in mice and reduced hepatotoxicity in vitro, as compared with 1. |
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