Highly potent 1,3-beta -D-glucan synthase inhibitors 10, 11 and 13 have bee
n identified by the chemical modification of the fungicidal macrocyclic lip
opeptidolactone, RO-09-3655 (1), isolated from the cultured broth of Deuter
omycotinia spp. D-Ornithine derivative (10) showed improved antifungal acti
vity in the systemic candidiasis model in mice and reduced hepatotoxicity i
n vitro, as compared with 1. (C) 2001 Elsevier Science Ltd. All rights rese
rved.