C-4:SUBSTITUTED MACROLIDE ANTIBIOTICS

摘要

This invention relates to compounds of the formula (see fig. I ) and to pharmaceutically acceptable salts thereof. The compounds of formula 1 arepotent antibacterial and antibacterial agents that m ay be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to met hods of treating bacterial and protozoal infections by administering the compounds of formula 1. In the formula, X is -CH(-NR18R A)-, -CO-, CH2NR9-, -NR9CH2 or -C(=NR5)-; R1 and R2 are each OH or R1 and R2 taken together repres ent -X2-CO-O-, or R1 is oxo, OH or NR9R10 and R2 and X1 taken together represent -O- etc.; R3 is OH or OCH3; R4 is -(CH2)n NR8R15; R20 is H or -COR9; R18 and R19 are each H, alkyl or the like; R9 is H or alkyl; R5 is OH, alkyl, alkoxy or the like; and X2 is -O-, -NR9- or -N(NR9R10)-.