| 摘要 |
The invention relates to antibacterial compounds of formula I;
wherein X is N or CH; R1 is H or halogen; R2 is alkynyloxy or the group M; R3 is H or halogen; M is one of the groups MA and MB represented below
;
wherein A is a bond, CH2CH2, CH═CH or C≡C; R1A is H or halogen; R2A is H, alkoxy or halogen; R3A is H, alkoxy, hydroxyalkoxy, alkoxyalkoxy, thioalkoxy, trifluoromethoxy, amino, hydroxyalkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxyalkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-ylalkoxy, morpholin-4-yl-alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, 1-hydroxymethyl-cycloprop-1-yl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 3-hydroxyoxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl, 1-(2-aminoacetyl)azetidin-3-yl, 1-glycylazetidin-3-yl, 1-(2-amino-2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl or 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl; and salts thereof. |
| 主权项 |
1. A compound of formula Iwherein
X represents N or CH; R1 represents H or halogen; R2 represents (C3-C4)alkynyloxy or the group M; R3 represents H or halogen; M is one of the groups MA and MB represented belowwherein A represents a bond, CH2CH2, CH═CH or C≡C;
R1A represents H or halogen; R2A represents H, (C1-C3)alkoxy or halogen; R3A represents H, (C1-C3)alkoxy, hydroxy(C1-C4)alkoxy, (C1-C3)alkoxy(C2-C3)alkoxy, (C1-C3)thioalkoxy, trifluoromethoxy, amino, hydroxy(C1-C4)alkyl, 2-hydroxyacetamido, 1-aminocyclopropyl, 1-hydroxymethyl-cycloprop-1-yl, 1-((phosphonooxy)methyl)cyclopropyl, 1-(((dimethylglycyl)oxy)methyl)cyclopropyl, trans-2-hydroxymethyl-cycloprop-1-yl, 1,2-dihydroxyethyl, 3-hydroxyoxetan-3-yl, 3-(hydroxy(C1-C3)alkyl)oxetan-3-yl, 3-aminooxetan-3-yl, 3-hydroxythietan-3-yl, morpholin-4-yl(C2-C3)alkoxy, morpholin-4-yl-(C1-C2)alkyl, oxazol-2-yl or [1,2,3]triazol-2-yl; and R1B represents hydroxy(C1-C3)alkyl, dihydroxy(C1-C4)alkyl, amino(C1-C3)alkyl, (dimethylamino)methyl, 1-hydroxymethyl-cycloprop-1-yl, trans-2-(1,2-dihydroxyethyl)cycloprop-1-yl, 1-methyl-2-hydroxymethyl-cycloprop-1-yl, 2-(hydroxymethyl)-2-methylcyclopropyl, 1-aminomethyl-cycloprop-1-yl, trans-2-hydroxymethyl-cycloprop-1-yl, 1-fluoro-2-(hydroxymethyl)cyclopropyl, 2-fluoro-2-(hydroxymethyl)cyclopropyl, 1-(hydroxymethyl)cyclobutyl, 3-hydroxyoxetan-3-yl, 3-hydroxymethyl-oxetan-3-yl, 3-hydroxythietan-3-yl, 1-(2-hydroxyacetyl)azetidin-3-yl, 1-(2-aminoacetyl)azetidin-3-yl, 1-glycylazetidin-3-yl, 1-(2-amino-2-methylpropanoyl)azetidin-3-yl, 3-(2-aminoacetamido)cyclopentyl, trans-(cis-3,4-dihydroxy)-cyclopent-1-yl, 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl, 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl, piperidin-4-yl, 1-(2-hydroxyacetyl)piperidin-4-yl, 4-hydroxytetrahydro-2H-pyran-4-yl, 5-aminotetrahydro-2H-pyran-2-yl, (1s,3r)-(1-hydroxy-3-(hydroxymethyl)cyclobutyl)methyl or 3-hydroxyoxetan-3-ylmethyl; or a salt thereof. |
