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    Metronidazole derivatives as antiparasitic agents
    3.
    发明公开
    Metronidazole derivatives as antiparasitic agents 有权
    甲硝唑衍生物抗寄生虫

    公开(公告)号：EP2085394A2

    公开(公告)日：2009-08-05

    申请号：EP09250251.7

    申请日：2009-01-30

    申请人： Legal Affairs Office University of Jordan

    发明人： Abu Shairah, Eman Ahmad Mohammad ,  Saadeh, Haythem Ali Mohammad ,  Mosleh, Ibrahim Mousa Ibrahim ,  Al Arif, Mikidad Tawfig Ayoub ,  Mubarak, Mohammad Suleiman (Al Haj M.)

    IPC分类号： C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4164 ,  A61K31/4184 ,  A61P31/04 ,  A61P33/02 ,  C07D233/92 ,  A61K31/423 ,  A61K31/428

    CPC分类号： C07D233/88 ,  C07D233/92 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： 2-methyl-5-nitro-imidazolyl compounds with the general formula I, II or III:

    wherein one of the groups R 1 , R 2 , R 3 , R 4 , R 5 is selected from an aldehyde and a 5- or 6-membered aromatic heterocylic group having 1 to 3 heteroatoms selected from N, O, S wherein the aromatic heterocylic group is optionally substituted and is optionally fused with a benzene ring that is optionally substituted; and each of the other groups R 1 , R 2 , R 3 , R 4 , R 5 is independently selected from hydrogen, alkyl, alkenyl, alkoxy, amino, alkylamino, dialkylamino, aryl, aralkyl, carboxyl, carboxylic ester, cyano, amido, bromo, chloro, fluoro, alkylamido and heterocyclic optionally substituted; R 6 is selected from - SO 2 -R 16 , -(CH 2 ) n -R 17 ; R 16 is a heterocylic group optionally substituted; R 17 is a heterocylic group optionally substituted; n is selected from 1 to 5; R 7 is selected from C2-C10 alkyl, aryl optionally substituted, heterocyclic optionally substituted, alkenyl and C2-C4 hydroxyalkyl; R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen and alkyl; the optionally substituted aryl, heterocyclic, aromatic heterocyclic groups and benzene rings are optionally substituted with one or more groups independently selected from alkyl, alkenyl, alkoxy, amino, alkylamino, dialkylamino, carboxyl, carboxylic ester, cyano, amido, bromo, chloro, fluoro and alkylamido. These compounds are used as antiparasitic and antibacterial agents.

    摘要翻译： 具有通式I，II或III的2-甲基-5-硝基 - 咪唑基化合物：其中基团R 1，R 2，R 3，R 4，R 5中的一个选自醛和5-或6 具有1至3个选自N，O，S的杂原子的芳族杂环基团，其中芳族杂环基团任选被取代，并任选地与任选被取代的苯环稠合; 并且R 1，R 2，R 3，R 4，R 5中的每一个独立地选自氢，烷基，烯基，烷氧基，氨基，烷基氨基，二烷基氨基，芳基，芳烷基，羧基，羧酸酯，氰基， ，溴，氯，氟，烷基酰氨基和杂环任选取代; R 6选自-SO 2 -R 16， - （CH 2）n -R 17; R 16是任选取代的杂环基团; R 17是任选取代的杂环基团; n选自1至5; R 7选自C 2 -C 10烷基，任选取代的芳基，任选取代的杂环，烯基和C 2 -C 4羟烷基; R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15各自独立地选自氢和烷基; 任选取代的芳基，杂环，芳族杂环基和苯环任选被一个或多个独立地选自烷基，烯基，烷氧基，氨基，烷基氨基，二烷基氨基，羧基，羧酸酯，氰基，酰氨基，溴，氯，氟 和烷基酰氨基。 这些化合物用作抗寄生虫和抗菌剂。