cas 499-78-5, 5-hydroxy-4-oxo-4H-pyran-2-carboxylic acid | Articles data ｜lookchem

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499-78-5

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Design, synthesis and biological evaluation of novel DNA gyrase inhibitors and their siderophore mimic conjugates
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
(2020/01/08)

A Convenient Preparation of Carboxy-γ-pyrone Derivatives: Meconic Acid and Comenic Acid
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Güntzel, Paul,Forster, Leonard,Schollmayer, Curd,Holzgrabe, Ulrike
p. 512 - 516
(2019/01/10)

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Chemical Properties

Melting Point: 284-294 °C
Boiling Point: 420.7 °C at 760 mmHg
Flash Point:187.7 °C
Density: 1.819 g/cm³
Vapor Pressure: 7.71E-09mmHg at 25°C
Refractive Index: 1.66
PSA: 87.74000
LogP: 0.04360

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