| 摘要 |
The invention relates to hydroxyphenyl derivatives of formula (I) wherein R1 is phenyl or a 6 membered monocyclic nitrogenous heteroaryl of formula wherein Z4, Z5, Z6, Z7 and Z8 are C or N with a maximum of three N, R1 being possibly substituted by 1 to 3 R identical or different, - R2 is phenyl, C-C alkyl, C-C alkenyl, C-C alkynyl, C- Cf luoro-alkyl, C-Cf luoro-alkenyl, OR, SR, all being possibly substituted by 1 to 3 identical or different R', - R,R and R, are H, C-C alkyl, C-C alkenyl, C-C alkynyl, phenyl, heteroaryl and aliphatic heterocycle as defined above for R2, the heteroaryl and the heterocycle being possibly formed with the carbon and nitrogen atoms to which R, R and R are linked, - R' is heteroaryl and aliphatic heterocycle as defined above for R2, C-C alkyl, CHCOR", COR", COR", CONR"R"', OCOR", OR", NR"R"', NR"C0R'", NR"COOR"', OCONR"R"', NR"CONR"R"', NR"SOR"', SOR", NR"SOR"', halogen and CN, R" and R"', identical or different, are H, C-C alkyl or form together a 4 to 6 membered heterocycle with 1 to 3 heteroatoms selected from N, 0 and S, - Y represents H or a labile chemical group able to regenerate in vivo the free phenol - Z1 and Z3 are halogen or H, and Z2 is fluor or H, provided that - either Z2 is fluor and all the other definitions are as defined above, - or Z6 is a carbon atom substituted by R as defined above, R being different from H, alkyl, halogen, NH2, OH, CONH or fluoro alkyl and all the other definitions are as defined above, - or Z4 or Z5, or Z7 or Z8 are carbon atoms substituted by NRR or OR, OR being different from OH and all the other definitions are as defined above, - or Z5, or Z7, is a carbon atom substituted by R, R being different from H and all the other definitions are as defined above, - or R2 is a C-Calkyl-heteroaryl radical or a C- Calkyl-OR radical, 0R being different from OH and all the other definitions are as defined above. Applications as anti-bacterial and/or anti-parasites agents. |
