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HYBRID AMIDES BASED ON TRIAZOLE AND THIAZOLIDINE HAVING ANTIMICROBIAL ACTIVITY

机译:基于三唑和噻唑烷的混合酰胺具有抗微生物活性

摘要

FIELD: medicine.;SUBSTANCE: invention relates to compounds of general formula (I) or a pharmaceutically acceptable salt thereof, where Z is independently selected and represents a fragment whose structural formula is given below, wherein the asterisk indicates an attachment point; X is independently selected and represents O or S; R1 is independently selected and represents a benzylidene moiety optionally containing 1–3 substituents R', which is independently selected and represent -C1-7-alkyl, -OC1-7-alkyl, halogen, -OH, -C5-7-cycloalkyl, -piperazinyl, optionally containing a substitute selected from -C1-7-alkyl; wherein the asterisk indicates the substitution attachment point; R2 is independently selected and represents H, -C1-7-alkyl, phenyl; said phenyl in fragment R2 is optionally substituted with at least two substitutes, which are halogen; R3 is independently selected and represents halogen; R4 is independently selected and represents halogen; n take values from 0 to 3. ; ;Z: , , , , , ;;R1: .;EFFECT: disclosed compounds are intended for treating and/or preventing an infectious disease of microbial aetiology in a subject caused by a fungal infection, wherein the disease of the microbial aetiology is caused by fungi of the genus Candida speciales, Aspergillus speciales, Microsporum speciales, Trichophyton speciales and/or Epidermophyton speciales.;13 cl, 5 tbl, 56 ex
机译:发明领域本发明涉及通式(I)的化合物或其药学上可接受的盐,其中Z是独立选择的并且代表其结构式如下所示的片段,其中星号表示连接点; X是独立选择的,代表O或S; R 1 是独立选择的,代表可任选包含1-3个取代基R'的亚苄基部分,R'独立选择并代表-C 1-7 -烷基,-OC < Sub> 1-7 -烷基,卤素,-OH,-C 5-7 -环烷基,-哌嗪基,可选包含选自-C 1-7 < / sub>-烷基;其中星号表示取代连接点; R 2 是独立选择的,代表H,-C 1-7 -烷基,苯基;片段R 2 中的苯基任选被至少两个卤素取代基取代; R 3 是独立选择的,代表卤素; R 4 是独立选择的,代表卤素; n取0到3之间的值。 ; Z:,<图像文件=“ 00000105.JPG” he =“ 6” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 9” />,<图像文件=“ 00000106.JPG” he =“ 6” imgContent =“未定义” imgFormat =“ JPEG” wi =“ 6” />,<图像文件=“ 00000107.JPG” he =“ 7” imgContent =“未定义” imgFormat =“ JPEG” wi =“ 5” />,<图像文件=“ 00000108.JPG” he =“ 7” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 6” /> ;; R 1 。;效果:公开的化合物用于治疗和/或预防由真菌感染引起的受试者的微生物病因感染性疾病,其中微生物病因疾病是由特殊念珠菌属,特殊曲霉属,特殊微孢子菌属,毛癣菌属和/或表皮癣菌属的真菌引起的; 13 cl ,5汤匙,56前

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