The Experts below are selected from a list of 129 Experts worldwide ranked by ideXlab platform
Francisco Gamarro - One of the best experts on this subject based on the ideXlab platform.
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Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes
Antimicrobial agents and chemotherapy, 2008Co-Authors: Carmen López-martín, José M. Pérez-victoria, Luis Alberto Vieira De Carvalho, Santiago Castanys, Francisco GamarroAbstract:Sitamaquine (WR6026), an 8-Aminoquinoline Derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3δ-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3δ-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
Mongkol Sukwattanasinitt - One of the best experts on this subject based on the ideXlab platform.
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An 8-Aminoquinoline Derivative as a molecular platform for fluorescent sensors for Zn(II) and Cd(II) ions
Journal of Luminescence, 2018Co-Authors: Kanokthorn Boonkitpatarakul, Atchareeporn Smata, Kantapong Kongnukool, Suphongphan Srisurichan, Kittipong Chainok, Mongkol SukwattanasinittAbstract:Abstract The amide Derivatives of 8-Aminoquinoline with two types of amino acid pendants, i.e. glycine and β-alanine, are evaluated for fluorescence sensing of various metal ions. In Tris-HCl aqueous buffer solution, the Derivative containing glycine exhibits selective fluorescence enhancement with Zn2+. The fluorescence turn-on signal at a longer wavelength is a result of the binding between N-8-aminoquinolinylglycinamide and Zn2+ which is promoted by the deprotonation of the amide proton. However, both Zn2+ and Cd2+ induce the turn-on signal in ethanol solution. X-ray crystallography of single crystals of both Zn2+ and Cd2+ complexes formed in ethanol reveals 1-D coordination polymer structures in which the metal ions are tethered with N and O of the amide groups. Simultaneous detection of Zn2+ and Cd2+ are possible by using paper chromatographic separation and the ligand as a visualizing agent. The fluorescence imaging of either Zn2+ or Cd2+ in plant tissue is demonstrated. The conjugation of the ligand with dimethylaminophenylacetylene effectively tunes the emission color of the ligand while retaining the sensing selectivity. Therefore, N-8-aminoquinolinylglycinamide is a simple yet effective binding probe for Zn2+ and Cd2+ with excellent fluorescence signal transduction.
Diego Muñoz-torrero - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-Aminoquinoline Derivatives as potent, selective, brain permeable antitrypanosomal agents.
Bioorganic & Medicinal Chemistry, 2016Co-Authors: Irene Sola, Albert Artigas, Martin C. Taylor, F. Javier Pérez-areales, Elisabet Viayna, M. Victòria Clos, Belén Pérez, Colin W. Wright, John M. Kelly, Diego Muñoz-torreroAbstract:Current drugs against human African trypanosomiasis (HAT) suffer from several serious drawbacks. The search for novel, effective, brain permeable, safe, and inexpensive antitrypanosomal compounds is therefore an urgent need. We have recently reported that the 4-Aminoquinoline Derivative huprine Y, developed in our group as an anticholinesterasic agent, exhibits a submicromolar potency against Trypanosoma brucei and that its homo- and hetero-dimerization can result in to up to three-fold increased potency and selectivity. As an alternative strategy towards more potent smaller molecule anti-HAT agents, we have explored the introduction of ω-cyanoalkyl, ω-aminoalkyl, or ω-guanidinoalkyl chains at the primary amino group of huprine or the simplified 4-Aminoquinoline analogue tacrine. Here, we describe the evaluation of a small in-house library and a second generation of newly synthesized Derivatives, which has led to the identification of 13 side chain modified 4-Aminoquinoline Derivatives with submicromolar potencies against T. brucei. Among these compounds, the guanidinononyltacrine analogue 15e exhibits a 5-fold increased antitrypanosomal potency, 10-fold increased selectivity, and 100-fold decreased anticholinesterasic activity relative to the parent huprine Y. Its biological profile, lower molecular weight relative to dimeric compounds, reduced lipophilicity, and ease of synthesis, make it an interesting anti-HAT lead, amenable to further optimization to eliminate its remaining anticholinesterasic activity.
Carmen López-martín - One of the best experts on this subject based on the ideXlab platform.
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Sitamaquine Sensitivity in Leishmania Species Is Not Mediated by Drug Accumulation in Acidocalcisomes
Antimicrobial agents and chemotherapy, 2008Co-Authors: Carmen López-martín, José M. Pérez-victoria, Luis Alberto Vieira De Carvalho, Santiago Castanys, Francisco GamarroAbstract:Sitamaquine (WR6026), an 8-Aminoquinoline Derivative, is a new antileishmanial oral drug. As a lipophilic weak base, it rapidly accumulates in acidic compartments, represented mainly by acidocalcisomes. In this work, we show that the antileishmanial action of sitamaquine is unrelated to its level of accumulation in these acidic vesicles. We have observed significant differences in sitamaquine sensitivity and accumulation between Leishmania species and strains, and interestingly, there is no correlation between them. However, there is a relationship between the levels of accumulation of sitamaquine and acidotropic probes, acidocalcisomes size, and polyphosphate levels. The Leishmania major AP3δ-null mutant line, in which acidocalcisomes are devoid of their usual polyphosphate and proton content, is unable to accumulate sitamaquine; however, both the parental strain and the AP3δ-null mutants showed similar sensitivities to sitamaquine. Our findings provide clear evidence that the antileishmanial action of sitamaquine is unrelated to its accumulation in acidocalcisomes.
Baodui Wang - One of the best experts on this subject based on the ideXlab platform.
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Highly selective and sensitive fluorescent nanosensor for zinc ions
Sensors and Actuators B: Chemical, 2011Co-Authors: Zheng-yin Yang, Zengchen Liu, Baodui WangAbstract:Abstract Iron oxide magnetic nanoparticles were covalently modified by a fluorescent 8-Aminoquinoline Derivative and formed an optical sensor to be used as a highly sensitive and selective Zn 2+ ions fluorescent nanosensor in aqueous solution at pH 7.0. The nanosensor was sufficiently characterized by physicochemical methods. The sensor can detect Zn 2+ ions in aqueous solution with a submicromolar sensitivity of 0.1 μM, and the interfering metal ions cannot influence its selectivity. MTT assay experiments indicated that the sensor showed no apparent cytotoxicity.