Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 1.
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.
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