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

Abstract To increase the therapeutic utility of C-18 side-chain bearing pseudomycin analogue 2 , we prepared additional analogues and prodrugs of 2 containing further modifications at various positions within its core structure. Each of the newly synthesized derivatives ( 10 – 15 ) exhibited reduced tail vein toxicity relative to the parent compound. Some of the new pseudomycin derivatives (e.g., 14 ) also showed improved in vivo antifungal activity relative to its corresponding parent compound.