1037734-72-7Relevant academic research and scientific papers
New fluorescent rosamine chelator showing promising antibacterial activity against Gram-positive bacteria
Novais, ?ngela,Moniz, Tania,Rebelo, Ana Rita,Silva, Ana M.G.,Rangel, Maria,Peixe, Luísa
, p. 341 - 349 (2018)
The restricted number of antibiotics to treat infections caused by common multidrug resistant bacterial pathogens in the clinical setting demands a continuous search for new molecules with antibacterial properties. Bacterial iron deprivation represents a
ALA hybrid 3-hydroxypyridone derivative as well as preparation method and application thereof
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, (2021/07/17)
The invention designs and synthesizes a novel anti-tumor active compound with iron chelating property and photosensitive activity based on the principles of reasonable drug design, drug-likeness and the like. The invention aims to provide a preparation me
Novel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1 H)-ones as Dual-Acting Biofilm Inhibitors of Pseudomonas aeruginosa
Liu, Jun,Hou, Jin-Song,Li, Yi-Bin,Miao, Zhi-Ying,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
, p. 10921 - 10945 (2020/11/09)
2-Heptyl-3-hydroxy-4(1H)-quinolone (PQS), a compound from P. aeruginosa, functions as both a quorum sensing (QS) regulator and a potent iron chelator to induce expression of pyoverdine and pyochelin which are involved in high-affinity iron transport syste
Efficient bifunctional gallium-68 chelators for positron emission tomography: Tris(hydroxypyridinone) ligands
Berry, David J.,Ma, Yongmin,Ballinger, James R.,Tavare, Richard,Koers, Alexander,Sunassee, Kavitha,Zhou, Tao,Nawaz, Saima,Mullen, Gregory E. D.,Hider, Robert C.,Blower, Philip J.
, p. 7068 - 7070 (2011/08/22)
A new tripodal tris(hydroxypyridinone) bifunctional chelator for gallium allows easy production of 68Ga-labelled proteins rapidly under mild conditions in high yields at exceptionally high specific activity and low concentration.
Synthesis, iron(III)-binding affinity and in vitro evaluation of 3-hydroxypyridin-4-one hexadentate ligands as potential antimicrobial agents
Xu, Bo,Kong, Xiao-Le,Zhou, Tao,Qiu, Di-Hong,Chen, Yu-Lin,Liu, Mu-Song,Yang, Rong-Hua,Hider, Robert C.
, p. 6376 - 6380 (2011/12/02)
Iron is a critical element for the survival of bacteria. We have designed and synthesized two novel 3-hydroxypyridin-4-one hexadentate ligands with high affinity for iron(III), which disrupt bacterial iron absorption. Biological studies demonstrate that these two chelators have significant inhibitory effect against both Gram-positive and Gram-negative bacteria, and therefore have potential as antimicrobial agents.
Targeting the lysosome: Fluorescent iron(III) chelators to selectively monitor endosomal/ lysosomal labile iron pools
Fakih, Sarah,Podinovskaia, Maria,Kong, Xiaole,Collins, Helen L.,Schaible, Ulrich E.,Hider, Robert C.
experimental part, p. 4539 - 4552 (2009/07/04)
Iron-sensitive fluorescent chemosensors in combination with digital fluorescence spectroscopy have led to the identification of a distinct subcellular compartmentation of intracellular redox-active "labile" iron. To investigate the distribution of labile iron, our research has been focused on the development of fluorescent iron sensors targeting the endosomal/lysosomal system. Following the recent introduction of a series of 3-hydroxypyridin-4-one (HPO) based fluorescent probes we present here two novel HPO sensors capable of accumulating and monitoring iron exclusively in endosomal/lysosomal compartments. Flow cytometric and confocal microscopy studies in murine macrophages revealed endosomal/lysosomal sequestration of the probes and high responsiveness toward alterations of vesicular labile iron concentrations. This allowed assessment of cellular iron status with high sensitivity in response to the clinically applied medications desferrioxamine, deferiprone, and deferasirox. The probes represent a powerful class of sensors for quantitative iron detection and clinical real-time monitoring of subcellular labile iron levels in health and disease.
Design, synthesis, and evaluation of novel 2-substituted 3-hydroxypyridin-4-ones: Structure-activity investigation of metalloenzyme inhibition by iron chelators
Liu, Zu D.,Kayyali, Reem,Hider, Robert C.,Porter, John B.,Theobald, Anthony E.
, p. 631 - 639 (2007/10/03)
A range of novel 3-hydroxypyridin-4-ones with different R2 substitutents has been synthesized for the investigation of the structure-activity relationship between the chemical nature of the ligand and the inhibitory activity of the iron-contain
