| abstract |
The present invention provides lincosamides of general formula I, (I) wherein R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, 0(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, 0(C1-C4 alkyl), 0(C1-C4 alkenyl), 0(C1-C4 alkynyl), NH 2 , N(C1-C4 alkyl) 2 , N(C1-C4 alkenyl) 2 , N(C1-C4 alkynyl) 2 ; and pharmaceutically acceptable salts thereof. Further provided is a method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances. |