60126-29-6Relevant articles and documents
Acridinium-conjugated aromatic heterocycles as highly potent FtsZ inhibitors: Design, synthesis, and biological evaluation
Chen, Weijin,Guo, Ting,Ma, Shutao,Ma, Yangchun,Song, Di,Zhang, Nan,Zhang, Shenyan
, (2022/03/15)
The epidemic of multidrug resistance (MDR) is a serious threat to public health, and new classes of antibiotics with novel mechanisms of action are in critical need. We rationally designed and efficiently synthesized three series of new chemical entities with potential antibacterial activity targeting filamenting temperature-sensitive mutant Z (FtsZ). Evaluation of these compounds against a panel of Gram-positive bacteria including MDR and vancomycin-resistant Enterococcus?strains indicated that most compounds showed enhanced antibacterial efficacy, comparable or even superior to the reference drugs. The newly synthesized compounds proved to be substrates of the Escherichia coli efflux pump AcrB, thus affecting the activity. Their structure–activity relationships?were summarized in detail. The most potent compound 10f quickly eliminated bacteria in a bactericidal mode, with low susceptibility to induce bacterial resistance. Further mechanistic studies with the BsFtsZ protein revealed that 10f functioned as an effective FtsZ inhibitor through altering the dynamics of FtsZ self-polymerization via a stimulatory mechanism, which leads to inhibition of cell division and cell death. Besides, 10f not only displayed no obvious cytotoxicity to mammalian cells but also had a high efficacy in a murine model of bacteremia in vivo. Regarded as a whole, our findings highlight 10f as a promising new FtsZ-targeting bactericidal agent.
Fluorescent dye, preparation method and applications thereof
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Paragraph 0165; 0168; 0169; 0171, (2019/10/01)
The invention belongs to the technical field of organic synthesis, and particularly relates to a fluorescent dye, a preparation method and applications thereof, wherein the fluorescent dye has a structural general formula represented by a formula I defined in the specification, X and Y are the same or different O, S, C(CH3)2 or NR6, R2 and R3 are the same or different hydrogen or functional groups, R1, R4, R5 and R6 are all functional groups, and Z is a negative ion. According to the present invention, the fluorescent dye has living cell membrane permeability, can be used for fluorescence imaging of living cell microstructures, and can obtain STED super-resolution fluorescence imaging, laser confocal imaging and other fluorescence imaging of living cells.
Promising near-infrared non-targeted probes: Benzothiazole heptamethine cyanine dyes
Okoh, Okoh Adeyi,Bisby, Roger H.,Lawrence, Clare L.,Rolph, Carole E.,Smith, Robert B.
, p. 42 - 56 (2014/01/06)
A series of benzothiazole heptamethine cyanine dyes have been synthesized and their photophysical properties evaluated in relation to their structural features. These have been compared against two classical probes of this type: Indocyanine Green (IGC) and New Indocyanine Green (IR-820). Growth inhibitory studies were also performed using a eukaryotic, unicellular organism, fission yeast Schizosaccharomyces pombe. Herein we highlight some potentially interesting candidates with improved fluorescence quantum yields when compared with ICG and IR-820.
