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1. (WO2018161979) LINCOSAMIDE DERIVATIVES, PREPARATION AND USE THEREOF AS ANTIMICROBIAL AGENT

Pub. No.:    WO/2018/161979    International Application No.:    PCT/CZ2018/050008
Publication Date: Fri Sep 14 01:59:59 CEST 2018 International Filing Date: Sat Mar 10 00:59:59 CET 2018
IPC: C07H 15/18
A61K 31/7056
A61P 31/04
Applicants: MIKROBIOLOGICKY USTAV AV CR, V. V. I.
Inventors: JANATA, Jiri
KAMENIK, Zdenek
KADLCIK, Stanislav
NAJMANOVA, Lucie
GAZAK, Radek
Title: LINCOSAMIDE DERIVATIVES, PREPARATION AND USE THEREOF AS ANTIMICROBIAL AGENT
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), NH2, 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.