SYNTHESIS AND ANTIFUNGAL ACTIVITY OF PRADIMICIN DERIVATIVES - MODIFICATIONS ON THE AGLYCONE PART

Synthesis and antifungal activity of pradimicin analogs modified on th e aglycone part is described. Upon modification studies at various sit es of the aglycone part using pradimicin A (PRM A), C-11 position was found to be the sole site to be modified without loosing antifungal ac tivity. Further modification studies at C-11 position were carried out with 11-OH derivative of pradimicin T1 (PRM T1) because of its easy a vailability. Among the compounds prepared, 11-demethoxy derivative of PRM A (12) and 11-O-ethyl (13) and 11-O-fluoroethyl (14) derivatives o f PRM T1 showed promising antifungal activity comparable to that of PR M A.