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    • 1. 发明申请
    • DIPHENYL ETHER ANTIMICROBIAL COMPOUNDS
    • 二苯醚类抗微生物化合物
    • WO2006137840A2
    • 2006-12-28
    • PCT/US2005/030011
    • 2005-08-23
    • RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORKTONGE, Peter, J.SULLIVAN, ToddJOHNSON, Francis
    • TONGE, Peter, J.SULLIVAN, ToddJOHNSON, Francis
    • A61K31/075C07C43/23
    • C07C43/295C07C43/23C07C205/38
    • The present invention is directed to compounds having the formula: wherein A 1 , A 3 , A 6 , and A 8 independently represent CH or N; A 2 represents N or C-­X 1 a - R 1 ; A 4 represents N or C-X 2 b -R 2 ; R 1 and R 2 independently represent H, or a hydrocarbon containing a minimum of one carbon atom and a maximum of twenty six carbon atoms, wherein the hydrocarbon is unsubstituted, or is substituted with one or more of -OH, -NH 2 , -SH, halo, or -COOH; X 1 and X 2 independently represent -O-, - S-, -NH-, -C(O)O-, -C(O)-, -C(O)NH-, or -SO 2 NH-; a and b independently represent 0 or 1, provided that when a and b are both 0, then R 1 and R 2 are not both H; when a is 1, then R 1 is not H; and when b is 1, then R 2 is not H; A 5 and A 9 independently represent CR 3 or N; R 3 represents H, methyl, ethyl, or halo; A7 represents CR 4 or N; R 4 represents H, methyl, ethyl, halo, nitro, hydroxy, amino, amido, or a methyl or ethyl group substituted with halo, nitro, hydroxy, amino, or amido; provided that A 2 and A 4 are not both N; and not more than three of A 5 , A 6 , A 7 , A 8 , and A 9 are N. The invention is also directed to pharmaceutical compositions comprising a compound according to (1) and a pharmaceutically acceptable carrier. The invention is also directed to methods of inhibiting the growth of a bacterium containing an enoyl reductase enzyme encoded by a fabI gene, a fabK gene, a fabL gene, or a combination thereof, in a mammal in need thereof, the method comprising administering to the mammal an effective amount of a compound according to formula (1).
    • 本发明涉及具有下式的化合物:其中A 1,A 3,A 6和A 8, SUP>独立代表CH或N; A 2表示N或C-X 1