发明名称 Fluorescent carbapenems
摘要 Chromogenic or fluorescent carbapenems according to formula I, wherein Ar is a mono or disubstituted carbocyclic aromatic group or an optionally mono or disubstituted heterocyclic aromatic group, are useful compounds for the detection of bacterial carbapenemase.;
申请公布号 US9296752(B2) 申请公布日期 2016.03.29
申请号 US201113806840 申请日期 2011.07.04
申请人 发明人 Pfaendler Hans Rudolf;Golz Gregor
分类号 C07D307/18;C12Q1/34;C07D477/14 主分类号 C07D307/18
代理机构 Locke Lord LLP 代理人 Locke Lord LLP ;DiCeglie, Jr. Nicholas J.
主权项 1. A method for detecting microbial carbapenem resistance, or detection of bacterial carbapenemase, the method comprising: contacting a fluorescent or chromogenic carbapenem of formula I  and/or its salts, wherein R1 is selected from hydrogen or alkyl and acyl, each with 1 to 6 carbon atoms and wherein Ar is a carbocyclic aromatic or heterocyclic aromatic group wherein the carbocyclic aromatic moiety is elected from phenyl, 1-biphenyl-2-yl or 1-biphenyl-4-yl and the heterocyclic aromatic moiety is selected from 2-pyridyl, 4-pyridyl or 2-pyrimidyl, and wherein the substituents R2 and R3 are selected, independently from each other, from hydrogen, amino, hydroxy, oxo, fluoro, chloro, bromo, nitro, cyano, carboxy, carbamoyl, sulphamoyl, amidino, guanidino, sulfo, or alkyl, alkoxy, acyl, acylamino, monoalkylamino, dialkylamino, trialkylammonium, N,N-dialkylcarbamoyl, N-alkylcarbamoyl and alkoxycarbonyl, each with 1 to 6 carbon atoms; wherein least one of R2 and R3 is an electron withdrawing group when Ar is a carbocylic aromatic group; and wherein R2 and R3 are not both hydrogen when Ar is a carbocylic aromatic group with a bacterium or a preparation obtained by lysis of at least one bacterial species; and detecting a change in color or fluorescence; wherein the change in color or fluorescence is indicative of microbial carbapenem resistance or the presence of bacterial carbapenemase.
地址 Stockdorf DE