| 摘要 |
Compounds of formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections: wherein R<1> is H, C1-6alkyl or Ar-C0-6alkyl; R<2> is H, C1-6alkyl, Ar-C0-6alkyl, HO-(CH2)n- or R'OC(O)-(CH2)n-; R<3> is A-C0-4alkyl, A-C2-4alkenyl, A-C2-4alkynyl, A-C3-4oxoalkenyl, A-C3-4oxoalkynyl, A-C1-4aminoalkyl, A-C3-4aminoalkenyl, A-C3-4aminoalkynyl, optionally substituted by any accessible combination of one or more of R<10> or R<7>; R<4> is (a), (b), (c), or (d); R<5> is H, C1-6alkyl, Ar-C0-6alkyl or C3-6cycloalkyl-C0-6alkyl; A is H, C3-6cycloalkyl, Het or Ar; R<7> is-COR<8>, -COCR'2R<9>, -C(S)R<8>, -S(O)kOR', -S(O)kNR'R'', -PO(OR'),-PO(OR')2, -B(OR')2, -NO2, or tetrazolyl; R<8> is -OR', -NR'R'', -NR'SO<2>R', or -NR'OR', -OCR'2CO(O)R'; R<9> is -OR', -CN, -S(O)rR', -S(O)kNR'2, -C(O)R', C(O)NR'2, or -CO2R'; R<10> is H, halo, -OR<11>, -CN, -NR'R<11>, -NO2, -CF3, CF3S(O)r-, -CO2R', -CONR'2, A-C0-6alkyl-, A-C1-6oxoalkyl-, A-C2-6alkenyl-, A-C2-6alkynyl-, A-C0-6alkyloxy-, A-C0-6alkylamino- or A-C0-6alkyl-S(O)r-; R<11> is R', -C(O)R', -C(O)NR'2, -C(O)OR', -S(O)kR', or -S(O)kNR'2; R' is H, C1-6alkyl, Ar-C0-6alkyl or C3-6cycloalkyl-C0-6alkyl; R'' is R', -C(O)R' or -C(O)OR'; R''' is H, C1-6alkyl, Ar-C0-6alkyl, HO-(CH2)2-, R'C(O)-, (R')2NC(O)CH2- or R'S(O)2-; X is H, C1-4alkyl, OR', SR', C1-4alkylsulfonyl, C1-4alkylsulfoxyl, -CN, N(R')2, CH2N(R')2,-NO2,-CF3, -CO2R', -CON(R')2, -COR', -NR'C(O)R', F, C1, Br, I, or CF3S(O)r-; k is 1 or 2; m is 1, 2 or 3; n is 1 to 6; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
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