| 摘要 |
Disclosed are 2-(aryloxy)-4-(heterocyclyl)-9H-pyrimido[4,5-b]indole derivatives of the general formula (I) or pharmaceutically suitable salts thereof, wherein L is O or S; R8 is H, Cl, Br, OH, amino, alkylamino, aminoalkyl, aminocyclopropyl, methoxy, ethoxy, cyclopropylamino, cyclopropylmethyl, chloromethyl, dichloromethyl, trichloromethyl, CH2CH2Cl, bromomethyl, dibromomethyl, fluoromethyl, difluoromethyl, trifluoromethyl, CH2CH2F, CH2CHF2, CH2CF3, NHOH, NHNHCH3, NHOCH3, NHCD3, SCH3 or NHCOH; X, Y and Z are CRX, CRY, and CRZ, respectively, wherein RX is H, methyl, Cl, Br or F; RY is H, methyl, difluoromethyl, trifluoromethyl, cyano, ethyl, Cl, Br, or F; Rz is H, methyl, Cl, Br, or F; R2 is an optionally substituted aryl as defined herein; and R4 is an optionally substituted aryl, optionally substituted aryloxy, substituted amino, or heterocycle connected through a nitrogen atom. Representative compounds include 6-fluoro-4-[(3aR,6aR)-hexahydropyrrolo[3,4-b]pyrrol-5(1H)-yl]-N-methyl-2-[(2-methylpyrimidin-5-yl)oxy]-9H-pyrimido[4,5-b]indol-8-amine. Also disclosed are pharmaceutical compositions comprising a compound as defined above for treating bacterial infections. |
