| abstract |
The present invention provides lincosamides of formula I wherein R 1 is selected from C 2 -C 8 alkyl, C 2 -C 8 alkenyl; R 3 is selected from OH, O (C 1 -C 4 alkyl), SH, S (C 1 -C 4 alkyl) or halogen; R 4 is H or C 1 -C 3 alkyl; each of R 21, R 22, R 23, R 24, R 25 is independently selected from the group consisting of H, OH, C 1 -C 4 alkyl, C 1 -C 4 alkenyl, C 1 -C 4 alkynyl, halogen, O (C 1 -C 4 alkyl), O (C 1-6 alkyl); C 4 alkenyl), O (C 1 -C 4 alkynyl), NH, N (C 1 -C 4 alkyl) N (C 1 -C 4 alkenyl), N (C 1 -C 4 alkynyl); and a pharmaceutically acceptable salt thereof. Also provided is a process for the preparation thereof, particularly a biosynthetic method utilizing the newly established functions of the Cetb1 and / or Cbb2 whole-cell biosynthetic proteins. The lincosamides of Formula I are suitable for use as antibacterial and antiprotozoal agents. |