主权项 |
1. A method of treatment of microbial infection which comprises administering to a patient in need thereof an effective amount of a hydroxyphenyl derivative of formula (I), wherein the microbial infection is an infection by bacteria carrying the FabI enzyme; R1 is phenyl R1 being optionally substituted by 1 to 3 R identical or different, R being selected from the group comprising H, fluoro, C1-C8 alkyl, C1-C4fluoro-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, COORa, CORa, CONRaRb, OCORa, CN, ORa, NRaRb, CRa═NORb, NRaCOORb, OCONRaRb, NRaCONRbRc, SRa, SO2Ra, SO2NRaRb, and NRaC(S)NRbRc, all being possibly substituted by R′, R2 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C4fluoro-alkyl, C2-C4fluoro-alkenyl, ORa, SRa, all being possibly substituted by 1 to 3 identical or different R′, Ra, Rb and Rc, identical or different, are selected from the group consisting of H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, R′ is selected from the group comprising C1-C8 alkyl, CH2CO2R″, CO2R″, COR″, CONR″R′″, OCOR″, OR″, NR″R′″, NR″COR′″, NR″COOR′″, OCONR″R′″, NR″CONR″R′″, NR″SO2R′″, SO2R″, NR″SO2R′″, halogen and CN, R″ and R′″, identical or different, are H or C1-C8 alkyl, Y represents H, Z1 and Z3, identical or different, are halogen or H, Z2 is fluoro, or a pharmaceutically acceptable organic or mineral salt, as well as the racemic derivatives and each unique not racemic derivatives, in case the derivatives of formula (I) have one or more chiral centers, both the cis (Z) and trans (E) isomers, in cases the derivatives of formula (I) have unsaturated carbon=carbon double bonds, and any N-oxide form of the derivatives. |