Imidazole, pyrazole, and triazole derivatives useful as antibacterial agentsThe present invention is directed to a new class of hydroxamic acid derivatives, their use as Lpx C inhibitors and, more specifically, their use to treat bacterial infections.The compound of formula iwhereinr 1(c 1-c 3) alkyl; r 2hydrogen or (c 1-c 3) alkyl; r 3hydrogen or (c 1-c 3) alkyl; x is n or cr 4; y is n or cr 4; r 4hydrogen or (c 1-c 3) alkyl; l is key, (c 2-c 6) alkenylene, (c 1-c 6) alkylidene group, (c 2-c 6) alkynylene ,-(ch 2) no (ch 2) p-,-(ch 2) ns (ch 2) p-,-(ch 2) nnr 5(ch 2) p-,-(ch 2) nso 2nr 5(ch 2) p-,-(ch 2) nnr 5so 2(ch 2) p-,-(ch 2) nconr 5(ch 2) p-or-(ch 2) nnr 5co (ch 2) p-; r 5and r 6hydrogen, (c independently 1-c 6) alkyl, (c 1-c 6) alkyl-carbonyl, (c 3-c 8) cycloalkyl, (c 3-c 8) cycloalkyl (c 1-c 6) alkyl or formyl radical; n is 0,1,2,3 or 4;p is 0,1,2,3 or 4;r 7(c 2-c 6) thiazolinyl, (c 1-c 6) alkoxyl group, (c 1-c 6) alkoxyl group (c 1-c 6) alkyl, (c 1-c 6) alkoxy carbonyl, (c 1-c 6) alkyl, (c 1-c 6) alkyl-carbonyl, (c 1-c 6) alkyl-nr 5-(c 1-c 6) alkyl, (c 1-c 6) alkylthio, (c 1-c 6) alkylthio (c 1-c 6) alkyl, (c 1-c 6) alkylthio carbonyl, (c 2-c 6) alkynyl, (c 6-c 12) aryl, (c 6-c 12) aryloxy, (c 6-c 12) arylthio, (c 6-c 12) aryl-nr 5-, cyano group, cyano group (c 1-c 6) alkyl, (c 5-c 8) cycloalkenyl group, (c 3-c 8) cycloalkyl, (c 3-c 8) cycloalkyloxy, (c 3-c 8) cycloalkylthio, (c 3-c 8) cycloalkyl-nr 5-, (c 5-c 12) heteroaryl, (c 5-c 12) heteroaryloxy, (c 5-c 12) heteroarylthio, (c 5-c 12) heteroaryl-nr 5-, (c 3-c 13) heterocycle, (c 3-c 13) heterocyclic oxy group, (c 3-c 13) heterocycle sulfenyl, (c 3-c 13) heterocycle-nr 5-, hydroxyl (c 1-c 10) alkyl, sulfydryl (c 1-c 6) alkyl, (nr 5r 6) alkyl or (nr 5r 6) carbonyl; and r 8for not existing, being (c 6-c 12) aryl, (c 6-c 12) aryl (c 1-c 6) alkyl, (c 3-c 8) cycloalkyl, (c 3-c 8) cycloalkyl (c 1-c 6) alkyl, (c 5-c 12) heteroaryl, (c 5-c 12) heteroaryl (c 1-c 6) alkyl, (c 3-c 13) heterocycle or (c 3-c 13) heterocycle (c 1-c 6) alkyl.
항박테리아제로서 유용한 이미다졸, 피라졸 및 트라이아졸 유도체본 발명은, 하이드록삼산 유도체의 신규 부류, LpxC 억제제로서 이의 용도, 보다 구체적으로 박테리아 감염을 치료하기 위한 이의 용도에 관한 것이다. 하기 화학식 I의 화합물:[화학식 I][이미지]상기 식에서,R1은 (C1-C3)알킬이고;R2는 수소 또는 (C1-C3)알킬이고;R3은 수소 또는 (C1-C3)알킬이고;X는 N 또는 CR4이고; Y는 N 또는 CR4이고;R4는 수소 또는 (C1-C3)알킬이고; L은 결합, (C2-C6)알켄일렌, (C1-C6)알킬렌, (C2-C6)알킨일렌, -(CH2)nO(CH2)p-, -(CH2)nS(CH2)p-, -(CH2)nNR5(CH2)p-, -(CH2)nSO2NR5(CH2)p-, -(CH2)nNR5SO2(CH2)p-, -(CH2)nCONR5(CH2)p- 또는 -(CH2)nNR5CO(CH2)p-이고; R5 및 R6은 독립적으로 수소, (C1-C6)알킬, (C1-C6)알킬카본일, (C3-C8)사이클로알킬, (C3-C8)사이클로알킬(C1-C6)알킬 또는 포름일이고; n은 0, 1, 2, 3 또는 4이고; p는 0, 1, 2, 3 또는 4이고; R7은 (C2-C6)알켄일, (C1-C6)알콕시, (C1-C6)알콕시(C1-C6)알킬, (C1-C6)알콕시카본일, (C1-C6)알킬, (C1-C6)알킬카본일, (C1-C6)알킬-NR5-(C1-C6)알킬, (C1-C6)알킬티오, (C1-C6)알킬티오(C1-C6)알킬, (C1-C6)알킬티오카본일, (C2-C6)알킨일, (C6-C12)아릴, (C6-C12)아릴옥시, (C6-C12)아릴티오, (C6-C12)아릴-NR5-, 시아노, 시아노(C1-C6)알킬, (C5-C8)사이클로알켄일, (C3-C8)사이클로알킬, (C3-C8)사이클로알킬옥시, (C3-C8)사이클로알킬티오, (C3-C8)사이클로알킬-NR5-, (C5-C12)헤테로아릴, (C5-C12)헤테로아릴옥시, (C5-C12)헤테로아릴티오, (C5-C12)헤테로아릴-NR5-, (C3-C13)헤테로사이클, (C3-C13)헤테로사이클옥시, (C3-C13)헤테로사이클티오, (C3-C13)헤테로사이클-NR5-, 하이드록시(C1-C10)알킬, 머캅토(C1-C6)알킬, (NR5R6)알킬 또는 (NR5R6)카본일이고;R8은 부재하거나, (C6-C12)아릴, (C6-C12)아릴(C1-C6)알킬, (C3-C8)사이클로알킬, (C3-C8)사이클로알킬(C1-C6)알킬, (C5-C12)헤테로아릴, (C5-C12)헤테로아릴(C1-C6)알킬, (C3-C13)헤테로사이클 또는 (C3-C13)헤테로사이클(C1-C6)알킬이다.