- Design, synthesis and biological evaluation of novel DNA gyrase inhibitors and their siderophore mimic conjugates
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Bacterial DNA gyrase is an important target for the development of novel antibacterial drugs, which are urgently needed because of high level of antibiotic resistance worldwide. We designed and synthesized new 4,5,6,7-tetrahydrobenzo[d]thiazole-based DNA gyrase B inhibitors and their conjugates with siderophore mimics, which were introduced to increase the uptake of inhibitors into the bacterial cytoplasm. The most potent conjugate 34 had an IC50 of 58 nM against Escherichia coli DNA gyrase and displayed MIC of 14 μg/mL against E. coli ΔtolC strain. Only minor improvements in the antibacterial activities against wild-type E. coli in low-iron conditions were seen for DNA gyrase inhibitor – siderophore mimic conjugates.
- Baran?oková, Michaela,Cruz, Cristina D.,Ila?, Janez,Kikelj, Danijel,Lamut, Andra?,Ma?i?, Lucija Peterlin,Skok, ?iga,Tammela, P?ivi,Toma?i?, Tihomir,Zega, Anamarija,Zidar, Nace
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- NOVEL CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF
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The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Paragraph 0106
(2014/03/25)
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- ANTIBACTERIAL COMPOUNDS
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The present Invention relates to cephalosporin antibacterial compounds of Formula (!): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
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Page/Page column 80; 81
(2013/04/24)
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- NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Page/Page column 39; 40
(2012/10/23)
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- Cephalosporins, processes for their preparation and pharmaceutical compositions containing them
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Antibacterial agents have the formula (Ia) or are pharmaceutically acceptable salts or invivohydrolysable esters thereof: wherein R1 is an acyl group, in particular that of an antibacterially active cephalosporin; R2 is hydrogen, methoxy, or formamido; Y is S, SO, SO2, O or CH2; X is oxygen, sulphur, or -NH- and R4 is a group of the formula CO Z R5 wherein Z is -CH=CH-, -(CH2)n- or -NH-; n is 0, 1 or 2; and R5 is: wherein R6 and R7 are the same or different, each representing hydroxy or protected hydroxy and R8 is hydroxy, amino, halogen or carboxy. The use of the compounds of formula (Ia) and intermediates for their preparation are also disclosed.
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- Cephalosporins, process for their preparation, pharmaceutical compositions containing them and intermediates
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β-Lactam antibiotics are disclosed which have the formula (IA) or are pharmaceutically acceptable salts or pharmaceutically acceptable invivohydrolysable esters thereof: wherein Y is a 1-(optionally substituted amino)-1H-tetrazol-5-yl, 4-(optionally subst
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