Synthesis and evaluation of novel pseudomycin side-chain analogues. Part 3

To increase the therapeutic utility of C-18 side-chain bearing pseudomycin analogue 2, we prepared additional analogues and prodrugs of 2 containing f urther modifications at various positions within its core structure. Each o f the newly synthesized derivatives (10-15) exhibited reduced tail vein tox icity relative to the parent compound. Some of the new pseudomycin derivati ves (e.g., 14) also showed improved in vivo antifungal activity relative to its corresponding parent compound. (C) 2001 Elsevier Science Ltd. All righ ts reserved.