- The Synthesis and Characterization of s-Triazine-Cored Tripodal Structure and Its Salen/Salophen-Bridged Fe/Cr(III) Capped Complexes
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A novel Schiff base compound was synthesized, and its complexation properties with Fe(III) and Cr(III) were investigated. Tripodal ligand was synthesized by the reaction of s-triazine and 4-hydroxybenzaldehyde. Then a Schiff base involving 8-hydroxyquinoline was synthesized by the reaction of 5-aminomethyl-8-hydroxyquinoline (QN) and 2,4,6-tris(p-formylphenoxy)-1,3,5-triazine (TRIPOD) in methanol/chloroform media. The obtained Schiff base (QN-TRIPOD) was then reacted with four trinuclear Fe(III) and Cr(III) complexes including tetradentate Schiff bases N,N′-bis(salicylidene)ethylenediamine (salenH2)/bis(salicylidene)-o-phenylenediamine (SalophenH2). The synthesized ligand and complexes were characterized by means of elemental analysis carrying out1H NMR, FTIR spectroscopy, thermal analyses, and magnetic susceptibility measurements. Finally, metal ratios of the prepared complexes were determined by using atomic adsorption spectrometry.
- Karatas, Erhan,Ucan, Halil Ismet
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- A Fluorescent Sensor for Al(III) and Colorimetric Sensor for Fe(III) and Fe(II) Based on a Novel 8-Hydroxyquinoline Derivative
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A novel 8-hydroxyquinoline-based fluorescent and colorimetric chemosensor was designed, synthesized and fully characterized. The sensor showed high selectivity and sensitivity toward Al3+ over other tested cations in EtOH/H2O (1:99, v/v) medium. The increase in fluorescence intensity was linearly proportional to the concentration of Al3+ with a detection limit of 7.38?×?10?6?M. Moreover, the sensor exhibited an obvious color change from yellow to black in the presence of Fe2+ and Fe3+ in EtOH/THF (99:1, v/v) solution. The absorbance changes showed a linear response to iron ions with the detection limits of 4.24?×?10?7?M and 5.60?×?10?7?M for Fe2+ and Fe3+, respectively. Thus, this chemosensor provides a novel approach for selectively recognition of Al3+, Fe3+ and Fe2+ among environmentally relevant metal ions.
- Lashgari, Negar,Badiei, Alireza,Mohammadi Ziarani, Ghodsi
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- Synthesis, characterization and application of uranyl ion imprinted polymers of aniline and 8-hydroxy quinoline functionalized aniline
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In this work we report a simple method for the synthesis of uranyl ion imprinted and non imprinted polyaniline (IPAN and NIPAN) and a copolymer of 8-hydroxyquinoline functionalized aniline (ANHQ) and aniline (IFPAN and NIFPAN) using potassium dichromate and ammonium persulphate as the initiators. The structural characterization of the synthesized materials was done by FTIR and UV-Visible spectroscopy, morphology by SEM, thermal properties by TG and electrochemical properties by cyclic voltammetry. Application of the synthesized materials in removal of uranyl ion was studied using solid phase extraction (SPE). Various parameters were optimized to get quantitative removal from aqueous samples buffered to neutral pH using ammonium acetate. Selectivity and reusability studies were carried out to demonstrate the possible application in real sample analysis.
- Milja,Krupa,Rao
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- Novel 8-hydroxyquinoline derivatives targeting β-amyloid aggregation, metal chelation and oxidative stress against Alzheimer's disease
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A series of multitargeted 8-hydroxyquinoline derivatives were designed and synthesized for the treatment of Alzheimer's disease (AD). In vitro studies indicated that most of the prepared compounds exhibited significant inhibitory effects against self-induced Aβ1?42 aggregation and potential antioxidant properties especially compound 5b (IC50 = 5.64 μM for self-induced Aβ aggregation; the oxygen radical absorbance capacity using fluorescein (ORAC-FL) value is 2.63 Trolox equivalents). Notably, 5b can chelate biometals and inhibit Cu2+/Zn2+-induced Aβ1?42 aggregation. The cell assays showed that 5b had excellent protective effects against oxidative toxin H2O2 and presented low neurotoxicity in PC12 cells. Furthermore, 5b could penetrate the blood–brain barrier (BBB) in vitro and did not show any acute toxicity in mice at doses up to 2000 mg/kg in vivo. Our findings provide a rationale for the potential application of compound 5b as a lead compound in AD therapy.
- Yang, Xuelian,Cai, Pei,Liu, Qiaohong,Wu, Jiajia,Yin, Yong,Wang, Xiaobing,Kong, Lingyi
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- Influence of metal coordination on the mismatch tolerance of ligand-modified PNA duplexes
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Recent studies on metal incorporation in ligand-modified nucleic acids have focused on the effect of metal coordination on the stability of metal-containing duplexes or triplexes and on the metal binding selectivity but did not address the effect of the sequence of the nucleic acid in which the ligands are incorporated. We have introduced 8-hydroxyquinoline Q in 10-mer PNA strands with various sequences and have investigated the properties of the duplexes formed from these strands upon binding of Cu2+. Variable-temperature UV-vis spectroscopy shows that, in the presence of Cu 2+, duplexes are formed even from ligand-modified Q-PNA strands that have a large number of mismatches. Spectrophotometric titrations demonstrate that at any temperature, one Cu2+ ion binds a pair of Q-PNA strands that each contain one 8-hydroxyquinoline, but below the melting temperature, the PNA duplex exerts a supramolecular chelate effect, which prevents the transformation in the presence of excess Cu2+ of the 1:2 Cu 2+:Q-PNA complexes into 1:1 complexes. EPR spectroscopy gives further support for the existence in the duplexes of [CuQ2] moieties that are similar to the corresponding square planar synthetic complex formed between Cu2+ and 8-hydroxyquinoline. As PNA duplexes show a preferred handedness due to the chiral induction effect of a C-terminal L-lysine, which is transmitted through stacking interactions within the duplex, only if the metal-containing duplex has complementary strands, does it show a chiral excess measured by CD spectroscopy. The strong effect of the metal-ligand moiety is suggestive of an increased correlation length in PNA duplexes that contain such moieties. These results indicate that strong metal-ligand alternative base pairs significantly diminish the importance of Watson-Crick base pairing for the formation of a stable PNA duplex and lead to high mismatch tolerance, a principle that can be used in the construction of hybrid inorganic-nucleic acid nanostructures.
- Watson, Richard M.,Skorik, Yury A.,Patra, Goutam K.,Achim, Catalina
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- Computational and experimental studies on the effect of conformational flexibility on bonding and photophysics of a triaza-macrocycle tripod
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The effect of conformational flexibility on coordination and bonding of a chelator, [12N3Me5Ox], on the macrocyclic ring 1,5,9-tris(-5-methylene)-1,5,9-triazadodecane and its lanthanide complexes is depicted by synthesis, characterization, and theoretical techniques. The chelator and its complexes were prepared and characterized by physicochemical methods. Each lanthanide complex was eight coordinated with a pseudo-C3 symmetric distorted dodecahedron geometry. Density functional theory (DFT) studies suggest that Ln3+ ions can be easily incorporated into the chelator cavity without changing the basic geometry. Natural bonding orbitals (NBO) and energy decomposition analysis (EDA) indicate that M–L bonds have ~ 70% ionic character. Exciting and diverse behavior was observed when the results of 12N3Me5Ox were compared with 9N3Me5Ox; with the increase in the size of the macrocyclic ring, the covalency of the metal–ligand bond was increased. The luminescence properties of these complexes were different in the solid and solution state. The f–f transitions of the lanthanide were not observed for the complexes. The theoretical results are in good agreement with the experiments.
- Verma, Rohini,Baral, Minati,Kanungo
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- Fluorescence-enhanced optical sensor for detection of Al3+ in water based on functionalised nanoporous silica type SBA-15
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An organic-inorganic hybrid optical sensor (PQ-SBA-15) was designed and prepared through functionalisation of the SBA-15 surface with 3-piperazinepropyltriethoxysilane followed by covalently attaching 8-hydroxyquinoline. Characterisation techniques, including FT-IR, thermal gravimetric, N2 adsorption-desorption and X-ray powder diffraction analyses, showed that the organic moieties were successfully grafted onto the surface of SBA-15 without the SBA-15 structure collapsing. The evaluation of the sensing ability of PQ-SBA-15 using fluorescence spectroscopy revealed that the PQ-SBA-15 was a selective fluorescence enhancement-based optical sensor for Al3+ in water in the presence of a wide range of metal cations including Na+, Mg2+, K+, Ca2+, Cr3+, Mn2+, Fe3+, Co2+, Ni2+, Cu2+, Zn2+, Cd2+, Hg2+ and Pb2+ with a limit of detection of 8.8 × 10-7 M. In addition, good linearity was observed between the fluorescence intensity and the concentration of Al3+.
- Karimi, Mehdi,Badieia, Alireza,Ziarani, Ghodsi Mohammadi
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- Green light material as well as preparation method and application thereof
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The invention belongs to the technical field of luminescent materials, and discloses a green light material and a preparation method and application thereof. The structural formula of the green light material is as follows: the fifth site of an 8-hydroxyquinoline structure is modified, a styryl structure is introduced, and the introduced styryl group can generate pi-pi conjugation with the 8-hydroxyquinoline structure, so that the electron cloud density of the 8-hydroxyquinoline structure is reduced; and meanwhile, by selecting metal ions and Zn , a new green light material is obtained, compared with traditional 8-hydroxyquinoline aluminum, the electron transport property is higher, the emission wavelength is subjected to red shift, the wavelength can be adjusted, and the color display requirement can be further met. Moreover, the green light material provided by the invention is good in thermal stability and high in color purity, and is a novel high-quality green light material.
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Paragraph 0032; 0037-0042
(2021/07/14)
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- Compound for promoting cell movement, pharmaceutical composition as well as preparation and application of compound
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The invention belongs to the field of medicinal chemistry, and particularly relates to a compound for promoting cell movement, a pharmaceutical composition and preparation and application thereof. The compound provided by the invention is 5-(isobutoxymethyl) quinoline-8-alcohol or 5-(isobutoxymethyl) quinoline-8-alcohol hydrochloride, and tests prove that the compound can promote the movement of NIH/3T3 and inhibit the movement of nasopharyngeal carcinoma cells CNE2 at the same time, has good safety, has a remarkable healing effect on skin wounds of mice, and can be used for preparing drugs for treating the skin wounds of the mice. The compound can be applied to preparation of drugs for promoting wound healing, is especially suitable for surgical patients with tumor combined with diabetes, can accelerate wound healing of the patients without causing tumor cell diffusion, and has extremely high medicinal potential.
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Paragraph 0016; 0033; 0035
(2021/07/10)
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- 8-hydroxyquinoline quaternary ammonium salt as well as preparation method and application thereof
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The invention discloses 8-Hydroxyquinoline quaternary ammonium salt as well as a preparation method and application thereof. The 8-Hydroxyquinoline quaternary ammonium salt is prepared from hydroxyquinoline (8-Hq), 18-tertiary amine and the like used as raw materials, structure and spectral properties are characterized, at the same time 8-Hq-CTAB is used as fluorescence probe to determine the critical micelle concentrations of several surfactants. The results show the 8-Hq-CTAB is sensitive to the microenvironment changes of nonionic and cationic surfactants and can be used to measure the critical micelle concentration, indicate the 8-Hq-CTAB is an ideal light switch for measuring the surfactant CMC. The 8-Hq-CTAB can not only be used as an ideal molecular light switch for the determination of the critical micelle concentration of the nonionic and cationic surfactants, but also can be used for the analysis of trace surfactants in the environment. The method is simple and easy to implement, and has good economic and social benefits.
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Paragraph 0041-0044
(2019/10/01)
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- Identification of Quinolinols as Activators of TEAD-Dependent Transcription
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The transcriptional co-regulators YAP (Yes-associated protein) and TAZ (transcriptional coactivator with PDZ-binding motif) are the vertebrate downstream effectors of the Hippo signaling pathway that controls various physiological and pathological processes. YAP and TAZ pair with the TEAD (TEA domain) family of transcription factors to initiate transcription. We previously identified a tractable pocket in TEADs, which has been physiologically shown to bind palmitate. Herein, a TEAD-palmitate interaction screen was developed to select small molecules occupying the palmitate-binding pocket (PBP) of TEADs. We show that quinolinols were TEAD-binding compounds that augment YAP/TAZ-TEAD activity, which was verified using TEAD reporter assay, RT-qPCR, and RNA-Seq analyses. Structure-activity relationship investigations uncovered the quinolinol substituents that are necessary for TEAD activation. We reveal a novel mechanism where quinolinols stabilize YAP/TAZ protein levels by occupying the PBP. The enhancement of YAP activity by quinolinols accelerates the in vivo wound closure in a mouse wound-healing model. Although small molecules that occupy the PBP have been shown to inhibit YAP/TAZ-TEAD activity, leveraging PBP to activate TEADs is a novel approach.
- Pobbati, Ajaybabu V.,Mejuch, Tom,Chakraborty, Sayan,Karatas, Hacer,Bharath, Sakshibeedu R.,Guéret, Stéphanie M.,Goy, Pierre-Alexis,Hahne, Gernot,Pahl, Axel,Sievers, Sonja,Guccione, Ernesto,Song, Haiwei,Waldmann, Herbert,Hong, Wanjin
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p. 2909 - 2921
(2019/12/24)
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- Wavelength-adjustable novel 8-hydroxyquinoline aluminum green-light material and preparation method thereof
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The invention belongs to the technical field of organic light-emitting materials and discloses a wavelength-adjustable novel 8-hydroxyquinoline aluminum green-light material and a preparation method thereof. The preparation method comprises the following steps: synthesis of an intermediate product CMQ, synthesis of an intermediate product SQ, and synthesis of a target product Al(SQ)3. The wavelength-adjustable novel 8-hydroxyquinoline aluminum green-light material and the preparation method disclosed by the invention have the advantages that by modification for 5 site of the 8-hydroxyquinolinestructure and introduction of a styryl structure with better conjugation and rigidity, the novel 8-hydroxyquinoline aluminum green-light material is good in heat stability, generates red shift of theemission wavelength, is also better in color purity, achieves the purpose of regulating the wavelength and is a better novel green-light material.
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Paragraph 0026; 0027
(2018/04/03)
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- Polymerizable 8-hydroxyquinoline aluminum salt green light material, and preparation method thereof
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The invention belongs to the technical field of luminescent material, and discloses a polymerizable 8-hydroxyquinoline aluminum salt green light material, and a preparation method thereof. According to the preparation method, 8-hydroxyquinoline, paraformaldehyde, and allyl alcohol are taken as raw materials, a series of reaction is adopted to introduce polymerizable groups to the 5th site of the structure of 8-hydroxyquinoline so as to obtain the polymerizable 8-hydroxyquinoline aluminum salt complex monomer. The solubility of polymerizable 8-hydroxyquinoline aluminum salt complex in organic solvents is improved, the polymerizable 8-hydroxyquinoline aluminum salt complex possesses polymerizability, and high molecular aluminium complex can be obtained through further polymerization; and inaddition, excellent heat stability is achieved. The novel complex possesses polymerizability, so that a novel approach is provided for synthesis of high molecular green light material with excellent performance.
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Paragraph 0025; 0032
(2018/10/19)
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- Study on Relationship Between Fluorescence Properties and Structure of Substituted 8-Hydroxyquinoline Zinc Complexes
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Organic light-emitting diodes (OLEDs) produced from 8-hydroxyquinoline metal complexes play a vital role in modern electroluminescent devices. In this manuscript, a series of 8-hydroxyquinoline derivatives were synthesized by different methods and their corresponding zinc metal complexes were prepared. The UV and fluorescence properties of the complexes were measured aiming to understand the effect of substituents at the quinoline ring on the fluorescence properties of the complexes. When the C-5 of 8-hydroxyquinoline was replaced by halogen group, the fluorescence emission wavelengths had been red-shifted, at the same time, blue-shifted of fluorescence emission wavelength was observed when the C-5 position of 8-hydroxyquinoline was substituted by electron-withdrawing group. When the C-4 position of 8-hydroxyquinolie was substituted by methyl or the C-5 position was substituted by sulfonic acid group, the corresponding zinc complexes had higher fluorescence intensity than 8-hydroxyquinolie zinc.
- Jianbo, He,Tingting, Zhou,Yongjing, Cao,Yuanyuan, Zhang,Weiqing, Yang,Menglin, Ma
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p. 1121 - 1126
(2018/08/17)
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- Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease
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A series of novel donepezil derivatives was designed, synthesized and evaluated as multifunctional acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer's disease (AD). The screening results indicated that most of the compounds exhibited potent inhibition of AChE with IC50values in the nanomolar range. Moreover, these derivatives displayed good antioxidant, Aβ interaction, blood-brain barrier penetration (PAMPA-BBB+) and ADMET properties (in silico). Among them, 5c demonstrated excellent AChE inhibition (IC50: 85?nM for eeAChE, 73?nM for hAChE), metal chelation, and inhibitory effects on self-induced, hAChE-induced and Cu2+-induced Aβ1-42aggregation (18.5%, 72.4% and 46.3%, at 20?μM). Kinetic analysis and molecular modeling studies suggested that 5c could bind simultaneously to the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. More importantly, 5c exhibited significant neuroprotective potency against Aβ1-42-induced PC12?cell injury. Furthermore, the step-through passive avoidance test showed 5c significantly reversed scopolamine-induced memory deficit and no hepatotoxicity in mice. These results indicated that 5c might be a promising drug candidate for AD therapy.
- Wang, Zhi-Min,Cai, Pei,Liu, Qiao-Hong,Xu, Ding-Qiao,Yang, Xue-Lian,Wu, Jia-Jia,Kong, Ling-Yi,Wang, Xiao-Bing
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supporting information
p. 282 - 297
(2016/08/04)
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- Multi-target-oriented protective agent neurocyte
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PROBLEM TO BE SOLVED: To provide a promising multi target direction type pharmaceutical candidate molecule which is promising for treatments of Alzheimer-type dementia (AD), which is a molecule having good cell membrane permeability including blood brain barrier.SOLUTION: A compound designed by a conjunction method with which a benzylpiperidine part of an acetylcholine esterase (AChE) inhibitor, donepezil is connected through an oligomethylene linker and combined with a propargyl part having a monoamine oxidase(MAO) inhibition activity and 8-hydroxy-5-methylaminoquinoline functional group, i.e. a center nitrogen atom substituted by a pro-chelator motif of a biochemical metal, interacts with AChE and butyrylcholinesterase(BuChE), further MAOA and B.
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Paragraph 0107-0109
(2017/03/28)
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- A fluorescent compound and based on the fluorescent compound fluorescent probe and visual preparation of test paper method and application
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The invention discloses a fluorescent compound and a fluorescent probe based on the fluorescent compound as well as a preparation method and an application of visible test paper, and belongs to the technical field of the preparation of the fluorescent compound. Cholesterol (cholic acid) and 8-hydroxyquinoline are respectively used as a side-chain structure and an end-capping structure to be simultaneously introduced into para-position di-benzyne substituted benzene so that a novel fluorescent compound is synthesized and has all supermolecule characteristics. The fluorescent probe prepared by utilizing the fluorescent compound is good in photochemical stability in a water phase and capable of high sensitively and selectively identifying sarin nerve gas and simulants thereof. The preparation method of the fluorescent compound is simple to operate and moderate in reaction condition; the prepared fluorescent probe is good in photochemical stability, high in sensitivity and good in selectivity; when the fluorescent molecular probe is combined with a commodity fluorescent instrument, the environmental sarin poison gas and simulants thereof can be sensitively detected.
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Paragraph 0115-0116
(2017/06/13)
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- Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease
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The synthesis, biochemical evaluation, ADMET, toxicity and molecular modeling of novel multi-target-directed Donepezil + Propargylamine + 8-Hydroxyquinoline (DPH) hybrids 1-7 for the potential prevention and treatment of Alzheimer's disease is described. The most interesting derivative was racemic α-aminotrile4-(1-benzylpiperidin-4-yl)-2-(((8-hydroxyquinolin-5-yl) methyl)(prop-2-yn-1-yl)amino) butanenitrile (DPH6) [MAO A (IC50 = 6.2 ± 0.7 μM; MAO B (IC50 = 10.2 ± 0.9 μM); AChE (IC50 = 1.8 ± 0.1 μM); BuChE (IC50 = 1.6 ± 0.25 μM)], an irreversible MAO A/B inhibitor and mixed-type AChE inhibitor with metal-chelating properties. According to docking studies, both DPH6 enantiomers interact simultaneously with the catalytic and peripheral site of EeAChE through a linker of appropriate length, supporting the observed mixed-type AChE inhibition. Both enantiomers exhibited a relatively similar position of both hydroxyquinoline and benzyl moieties with the rest of the molecule easily accommodated in the relatively large cavity of MAO A. For MAO B, the quinoline system was hosted at the cavity entrance whereas for MAO A this system occupied the substrate cavity. In this disposition the quinoline moiety interacted directly with the FAD aromatic ring. Very similar binding affinity values were also observed for both enantiomers with ChE and MAO enzymes. DPH derivatives exhibited moderate to good ADMET properties and brain penetration capacity for CNS activity. DPH6 was less toxic than donepezil at high concentrations; while at low concentrations both displayed a similar cell viability profile. Finally, in a passive avoidance task, the antiamnesic effect of DPH6 was tested on mice with experimentally induced amnesia. DPH6 was capable to significantly decrease scopolamine-induced learning deficits in healthy adult mice.
- Wang, Li,Esteban, Gerard,Ojima, Masaki,Bautista-Aguilera, Oscar M.,Inokuchi, Tsutomu,Moraleda, Ignacio,Iriepa, Isabel,Samadi, Abdelouahid,Youdim, Moussa B.H.,Romero, Alejandro,Soriano, Elena,Herrero, Raquel,Fernández Fernández, Ana Patricia,Ricardo-Martínez-Murillo,Marco-Contelles, José,Unzeta, Mercedes
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p. 543 - 561
(2014/06/09)
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- New multi-target-directed small molecules against Alzheimer's disease: A combination of resveratrol and clioquinol
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Alzheimer's disease (AD) is currently one of the most difficult and challenging diseases to treat. Based on the 'multi-target-directed ligands' (MTDLs) strategy, we designed and synthesised a series of new compounds against AD by combining the pharmacophores of resveratrol and clioquinol. The results of biological activity tests showed that the hybrids exhibited excellent MTDL properties: a significant ability to inhibit self-induced β-amyloid (Aβ) aggregation and copper(ii)-induced Aβ aggregation, potential antioxidant behaviour (ORAC-FL value of 0.9-3.2 Trolox equivalents) and biometal chelation. Among these compounds, (E)-5-(4-hydroxystyryl)quinoline-8-ol (10c) showed the most potent ability to inhibit self-induced Aβ aggregation (IC50 = 8.50 μM) and copper(ii)-induced Aβ aggregation and to disassemble the well-structured Aβ fibrils generated by self- and copper(ii)-induced Aβ aggregation. Note that 10c could also control Cu(i/ii)-triggered hydroxyl radical (OH) production by halting copper redox cycling via metal complexation, as confirmed by a Cu-ascorbate redox system assay. Importantly, 10c did not show acute toxicity in mice at doses of up to 2000 mg kg-1 and was able to cross the blood-brain barrier (BBB), according to a parallel artificial membrane permeation assay. These results indicate that compound 10c is a promising multifunctional compound for the development of novel drugs for AD. This journal is the Partner Organisations 2014.
- Mao, Fei,Yan, Jun,Li, Jianheng,Jia, Xian,Miao, Hui,Sun, Yang,Huang, Ling,Li, Xingshu
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p. 5936 - 5944
(2014/08/05)
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- Synthesis and characterization of 5-substituted 8-hydroxyquinoline derivatives and their metal complexes
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5-Aminomethyl-8-hydroxyquinoline (QN) was synthesized as a scaffold to generate dimers, trimers, and tetramer metalloquinolates. Starting from QN, a series of 5-substituted 8-hydroxyquinoline derivatives conjugated with small bioactive molecules were synthesized. Absorption and emission spectra indicate that these QN derivatives chelate well with metal ions, which may serve as a new platform to explore the applications of metalloquinolates for a variety of potential applications.
- Li, Lihua,Xu, Bing
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experimental part
p. 10986 - 10995
(2009/04/11)
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- Synthesis and anti-HIV properties of new hydroxyquinoline-polyamine conjugates on cells infected by HIV-1 LAV and HIV-1 BaL viral strains
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To find new derivatives that block different virus strains entry in cells bearing specific surface receptors represent an interesting challenge for medicinal chemists. Here, we report the synthesis and the anti-HIV properties of a new series of analogues based on the introduction of quinoline moiety on various polyamine backbones, including polyazamacrocycles. Three compounds 7, 8, and 10 of this series were found active on PBMCs cells infected by HIV-1 LAV or by HIV-1 BaL, in contrast the well-known reference compound 1a (AMD 3100) was found only active on HIV-1 LAV strain.
- Moret, Vincent,Dereudre-Bosquet, Nathalie,Clayette, Pascal,Laras, Younes,Pietrancosta, Nicolas,Rolland, Amandine,Weck, Clement,Marc, Sylvain,Kraus, Jean-Louis
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p. 5988 - 5992
(2007/10/03)
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- Surface functionalization of cadmium sulfide quantum-confined nanoclusters. 4. Formation and reactivity of an aniline surface quantum dot
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The preparation, characterization, properties, and reactivity of a novel quantum-confined CdS nanocluster containing a chemically active aniline surface are described, along with three general methods for the covalent attachment of a wide scope of molecular moieties to the cluster surface. The formation of facile covalent linkages via DCC mediated amidization, secondary amine formation, and thiourea condensation is discussed and, as the introduction of surface functionality is crucial for the eventual realization of molecular electronic devices fabricated from such nanoclusters, several derivatized nanoclusters bearing interesting chromophoric, fluorescent, electroactive, and chiroptical tethered species are described. All three derivatization techniques occur under very mild conditions that have been demonstrated not to disturb the integrity of the nanocluster core. The preparation, characterization, properties, and reactivity of a novel quantum-confined CdS nanocluster containing a chemically active aniline surface are described, along with three general methods for the covalent attachment of a wide scope of molecular moieties to the cluster surface. The formation of facile covalent linkages via DCC mediated amidization, secondary amine formation, and thiourea condensation is discussed and, as the introduction of surface functionality is crucial for the eventual realization of molecular electronic devices fabricated from such nanoclusters, several derivatized nanoclusters bearing interesting chromophoric, fluorescent, electroactive, and chiroptical tethered species are described. All three derivatization techniques occur under very mild conditions that have been demonstrated not to disturb the integrity of the nanocluster core.
- Veinot, Jonathan G.C.,Galloro, Josie,Pugliese, Linda,Bell, Valerie,Pestrin, Robert,Pietro, William J.
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p. 1530 - 1539
(2007/10/03)
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