- A Highly Selective and Sensitive Chemosensor for Colorimetric and Fluorescent Detection of Al3+ and Living Cell Imaging
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A colorimetric and fluorescent dual chemosensor for detecting Al3+, (E)-N′-((2-hydroxynaphthalen-1-yl)methylene)nicotinohydrazide (HNN), was developed by combining 2-hydroxy-1-naphthaldehyde with nicotinohydrazide. Addition of Al3+ to EtOH-H2O solution of HNN gives rise to a visible colour change from colourless to light blue and a significantly enhanced fluorescence. Other metal ions including Na+, K+, Ca2+, Mg2+, Mn2+, Co2+, Ni2+, Cu2+, Cr3+, Ag+, Pb2+, Zn2+, Cd2+, Hg2+, Fe2+, and Fe3+ have no or little effect on the specific response of HNN to Al3+. The binding mode of HNN-Al3+ complex was further clarified by electrospray ionisation mass spectrometry and 1H NMR titration experiments.
- Li, Xiao-Bo,Chen, Jia-Yi,Wang, En-Ju
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- Recognition of Al3+ based on a naphthalene-based "off-On" chemosensor in near 100% aqueous media
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An efficient fluorescent Al3+ sensor, 2-hydroxy-1-naphthylaldehyde nicotinoyl hydrazone (HL) has been designed and synthesized. The receptor shows "off-on" fluorescent responses toward Al3+ in near 100% aqueous media. Other relevant metal ions such as Li+, Na+, K+, Ca2+, Mg2+, Cu2+, Co2+, Mn2+, Ni2+, Zn2+, Ba2+, Fe2+, Cd2+, Hg2+, Pb2+, Sc3+, Fe3+, Cr3+ caused almost no fluorescence increase. The reason for this phenomenon is that the addition of Al3+ to the solution of HL induce the formation of a 1:1 stoichiometry of the binding mode of L-Al(III) which inhibits the excited-state intramolecular proton transfer (ESIPT) and photoinduced electron transfer (PET). More importantly, the reversibility of the recognition process of HL was performed by adding a Al3+ bonding agent Na2EDTA.
- Qin, Jing-Can,Yang, Zheng-Yin,Yang, Peng
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- Novel multifunctional iron chelators of the aroyl nicotinoyl hydrazone class that markedly enhance cellular NAD+/NADH ratios
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Background and Purpose: Alzheimer's disease (AD) is a multifactorial condition leading to cognitive decline and represents a major global health challenge in ageing populations. The lack of effective AD therapeutics led us to develop multifunctional nicot
- Braidy, Nady,Egan, Suhelen,Huang, Michael L. H.,Palanimuthu, Duraippandi,Richardson, Des R.,Salikin, Nor Hawani,Wu, Zhixuan
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- Structure-Guided Synthesis and Mechanistic Studies Reveal Sweetspots on Naphthyl Salicyl Hydrazone Scaffold as Non-Nucleosidic Competitive, Reversible Inhibitors of Human Ribonucleotide Reductase
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Ribonucleotide reductase (RR), an established cancer target, is usually inhibited by antimetabolites, which display multiple cross-reactive effects. Recently, we discovered a naphthyl salicyl acyl hydrazone-based inhibitor (NSAH or E-3a) of human RR (hRR) binding at the catalytic site (C-site) and inhibiting hRR reversibly. We herein report the synthesis and biochemical characterization of 25 distinct analogs. We designed each analog through docking to the C-site of hRR based on our 2.7 ? X-ray crystal structure (PDB ID: 5TUS). Broad tolerance to minor structural variations preserving inhibitory potency is observed. E-3f (82% yield) displayed an in vitro IC50 of 5.3 ± 1.8 μM against hRR, making it the most potent in this series. Kinetic assays reveal that E-3a, E-3c, E-3t, and E-3w bind and inhibit hRR through a reversible and competitive mode. Target selectivity toward the R1 subunit of hRR is established, providing a novel way of inhibition of this crucial enzyme.
- Huff, Sarah E.,Mohammed, Faiz Ahmad,Yang, Mu,Agrawal, Prashansa,Pink, John,Harris, Michael E.,Dealwis, Chris G.,Viswanathan, Rajesh
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p. 666 - 680
(2018/02/16)
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- METHOD OF MODULATING RIBONUCLEOTIDE REDUCTASE
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A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase modulator (RRmod), the amount being effective to inhibit neoplastic cell growth.
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Paragraph 00175
(2017/07/05)
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- Acylhydrazone derivative used for treating heart failure
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The invention belongs to the technical field of medicines, and relates to design and preparation method for acylhydrazone derivatives shown as a general formula I, and the acylhydrazone derivatives can be used for treating systolic heart failure comprising congestive heart failure.
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- Tin(IV) complexes with 2-hydroxybenz(2-hydroxynaphth)aldehyde nicotinoylhydrazones (H2Ns, H2Nnf). Molecular and crystal structures of [SnCl3(HNnf)] · 2DMF
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The reaction of SnCl4 with 2-hydroxybenz(2-hydroxynaphth)aldehyde nicotinoylhydrazones (H2Ns, H2Nnf) in CH3OH gave non-electrolyte complexes [SnCl3(HNs)] (I) and [SnCl3(HNnf)] (II), which w
- Shmatkova,Seifullina,Starikova
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p. 293 - 299
(2015/05/20)
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- Nicotinic acid benzylidene/phenyl-ethylidene hydrazides: Synthesis, antimicrobial evaluation and QSAR studies
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A series of nicotinic acid hydrazides (1-19) was synthesized and tested in vitro for antimycobacterial, antiviral, antibacterial and antifungal activities. The antimycobacterial activity results indicated that the presence of electron withdrawing halo groups improved the antimycobacterial activity. The antiviral evaluation showed that none of the synthesized derivatives inhibited the replication of viruses at subtoxic concentrations, except compounds 9 and 12. The antimicrobial screening results demonstrated that compounds having methoxy and 2-hydroxy naphthalene substituents were the most active ones against tested microbial strains. QSAR investigations revealed that multi-target QSAR models were found to be more effective in describing the antimicrobial activity than one-target QSAR models.
- Narang, Rakesh,Narasimhan, Balasubramanian,Sharma, Sunil,Sriram, Dharmarajan,Yogeeswari, Perumal,De Clercq, Erik,Pannecouque, Christophe,Balzarini, Jan
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p. 733 - 749
(2012/05/05)
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