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Compounds for inhibiting drug-resistant strains of HIV-1 integrase

机译:抑制HIV-1整合酶耐药菌株的化合物

摘要

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of:; embedded image wherein X is N, C(OH), or CH;Y is H or OH;each of Z1-Z5 is independently H or halogen;R4 is H, OH, NH2, NHR8, NR8R9 or R8;R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; andR8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen to which R8 and R9 are attached form an optionally-substituted heterocycle.
机译:一种在受试者中抑制抗药性HIV-1整合酶的方法,该方法包括给予有需要的受试者治疗有效量的式I化合物或其药学上可接受的盐或酯,其结构为: “嵌入式图像” 其中X是N,C(OH)或CH;Y为H或OH;Z 1 -Z 5 各自独立地为H或卤素;R 4 是H,OH,NH 2 ,NHR 8 ,NR 8 R 9 或R 8 ;R 5 ,R 6 和R 7 各自独立地为H,卤素,OR 8 ,R 8 ,NHR 8 ,NR 8 R 9 ,CO 2 R 8 ,CONR 8 R 9 ,SO 2 NR 8 R 9 或R 5 和R 6 以及与R 5 和R 6 连接的碳原子一起形成任选取代的碳环或任选取代的杂环;和R 8,S 9分别独立地为H,任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的芳基,任选取代的环烷基,任选取代的亚环烷基,可选被取代的杂环,可选被取代的酰胺,可选被取代的酯或R 8 和R 9 与氮一起被R 8 和R 9 连接成一个可选取代的杂环。

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