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André Felipe Cândido da Silva et al.
Medical history, 58(1), 1-26 (2013-12-18)
This article addresses the discussion about quinine-resistant malaria plasmodium in the early decades of the twentieth century. Observed by Arthur Neiva in Rio de Janeiro in 1907, the biological and social resistance of malaria sufferers to preventive and curative treatment
Elisabet Lázaro et al.
Journal of medicinal chemistry, 51(7), 2009-2017 (2008-03-20)
We report here a new, label-free approach to measure serum protein binding constants. The assay is able to measure HSA K d values in the milli-molar to micromolar range. The protein is not immobilized on any surface and the assay
Yanpeng Hou et al.
Bioorganic & medicinal chemistry, 17(7), 2871-2876 (2009-03-14)
Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of the bark of Scutia myrtina led to the isolation of three new anthrone-anthraquinones, scutianthraquinones A, B and C (1-3), one new bisanthrone-anthraquinone, scutianthraquinone D (4), and the known anthraquinone
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Sanna R Rijpma et al.
Malaria journal, 13, 359-359 (2014-09-15)
Therapeutic blood plasma concentrations of anti-malarial drugs are essential for successful treatment. Pharmacokinetics of pharmaceutical compounds are dependent of adsorption, distribution, metabolism, and excretion. ATP binding cassette (ABC) transport proteins are particularly involved in drug deposition, as they are located
Marc C Tahita et al.
Malaria journal, 14, 251-251 (2015-06-20)
Ex vivo assays are usually carried out on parasite isolates collected from patients with uncomplicated Plasmodium falciparum malaria, from which pregnant women are usually excluded as they are often asymptomatic and with relatively low parasite densities. Nevertheless, P. falciparum parasites
Bin Shen et al.
Chirality, 25(9), 561-566 (2013-06-27)
New chiral phosphoramide ligands derived from cinchona alkaloids were developed, which react with diethylzinc to form chiral phosphoramide-Zn(II) complexes containing two Lewis bases and one Lewis acid. These trifunctional complexes can serve as highly efficient chiral catalysts for triple activation
Yupeng Sun et al.
Biomedical chromatography : BMC, 29(12), 1893-1900 (2015-05-23)
m-Nisoldipine, as a novel 1,4-dihydropyridine calcium ion antagonist, was presented as a couple of enantiomers [(-), (+)-m-nisoldipine]. In this report, the in vitro metabolism of m-nisoldipine enantiomers was investigated in rat liver microsomes (RLM) by the combination of two liquid
Diego Correia et al.
Psychopharmacology, 232(15), 2731-2739 (2015-03-24)
We hypothesized that the corticotropin-releasing factor (CRF) system is hyperresponsive in animals with high ethanol intake, which exhibits a reduction of ethanol intake when administered with a CRF1 receptor antagonist. Outbred Swiss mice were subjected to a long-term, three-bottle, free-choice
William J Horton et al.
Psychopharmacology, 232(14), 2519-2530 (2015-02-24)
While it is known that tobacco use varies across the 24-h day, the time-of-day effects are poorly understood. Findings from several previous studies indicate a potential role for melatonin in these time-of-day effects; however, the specific underlying mechanisms have not
Annemarie R Kreeftmeijer-Vegter et al.
Malaria journal, 12, 115-115 (2013-03-30)
Exchange transfusion (ET) has remained a controversial adjunct therapy for the treatment of severe malaria. In order to assess the relative contribution of ET to parasite clearance in severe malaria, all patients receiving ET as an adjunct treatment to parenteral
E Bezati et al.
Lupus, 24(1), 32-41 (2014-08-21)
Quinine, a quinoline derivative, is an ancient antipyretic drug with antimalarial properties that has been phased out by more effective synthetic candidates. In previous studies we discovered that hydroxychloroquine (HCQ), a synthetic antimalarial with structural similarities to quinine, reduced the
Francisco J Prado-Prado et al.
Bioorganic & medicinal chemistry, 18(6), 2225-2231 (2010-02-27)
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against
Le Ngoc Tran et al.
Journal of chromatography. A, 1396, 140-147 (2015-04-22)
A weak anion-exchanger chiral selector, quinine-incorporated silica/zirconia hybrid monolithic (QUI-S/ZHM) capillary column was prepared by sol-gel technology. The performance of the QUI-S/ZHM column was investigated for enantioresolution of a set of acidic chiral drugs and dinitrobenzoyl (DNB)-amino acids by capillary
Malaria during pregnancy with parasite sequestration in the villous chamber.
Armin Rashidi et al.
Blood, 121(12), 2173-2173 (2013-05-02)
Hao Meng et al.
Antimicrobial agents and chemotherapy, 54(10), 4306-4313 (2010-07-21)
Quinine resistance (QNR) in Plasmodium falciparum has been detected in many regions of the world where malaria is endemic. Genetic polymorphisms in at least four genes are implicated in QN susceptibility, and their significance often depends on the genetic background
Adriana Huertas et al.
Pharmacology, biochemistry, and behavior, 129, 26-33 (2014-12-09)
The Na(+)-dependent dopamine transporter (DAT) is primarily responsible for regulating free dopamine (DA) concentrations in the brain by participating in the majority of DA uptake; however, other DA transporters may also participate, especially if cocaine or other drugs of abuse
Paul M O'Neill et al.
Journal of medicinal chemistry, 52(7), 1828-1844 (2009-03-17)
On the basis of a mechanistic understanding of the toxicity of the 4-aminoquinoline amodiaquine (1b), three series of amodiaquine analogues have been prepared where the 4-aminophenol "metabolic alert" has been modified by replacement of the 4'-hydroxy group with a hydrogen
Li Ni-Komatsu et al.
Molecular pharmacology, 74(6), 1576-1586 (2008-09-20)
A series of quinolines, including chloroquine and quinine, were identified as potent pigmentation inhibitors through screening a compound library in murine melanocytes. Structure-activity relationship analysis indicated that 4-substituted amino groups with a tertiary amine side chain, such as chloroquine, were
Jacob D Johnson et al.
Antimicrobial agents and chemotherapy, 51(6), 1926-1933 (2007-03-21)
Several new fluorescence malaria in vitro drug susceptibility microtiter plate assays that detect the presence of malarial DNA in infected erythrocytes have recently been reported, in contrast to traditional isotopic screens that involve radioactive substrate incorporation to measure in vitro
Susan E Coldwell et al.
Neurology, 80(11 Suppl 3), S20-S24 (2013-04-23)
The NIH Toolbox for Assessment of Neurological and Behavioral Function (NIH Toolbox) is a set of brief measures for the assessment of cognitive function, emotional health, motor function, and sensory function for use in clinical trials and in epidemiologic and
Rafael M Palhares et al.
Journal of ethnopharmacology, 155(1), 815-822 (2014-06-28)
Quina is a popular name originally attributed to Cinchona pubescens Vahl (=Cinchona succirubra) and Cinchona. calisaya Wedd., species native from Peru that have the antimalarial alkaloid quinine. In Brazil, bitter barks substitutes for the Peruvian species began to be used
Yan Chen et al.
Current biology : CB, 24(17), 1969-1977 (2014-08-19)
Natural foods contain not only nutrients, but also nonnutritious and potentially harmful chemicals. Thus, animals need to evaluate food content in order to make adequate feeding decisions. Here, we investigate the effects of acids on the taste neuron responses and
Peter Starzengruber et al.
Malaria journal, 13, 228-228 (2014-06-12)
Spreading resistance of Plasmodium falciparum to existing drugs calls for the search for novel anti-malarial drugs and combinations for the treatment of falciparum malaria. In vitro and ex vivo investigations were conducted with fresh P. falciparum field isolates and culture-adapted
Maud Henry et al.
Antimicrobial agents and chemotherapy, 53(5), 1926-1930 (2009-03-11)
Polymorphisms in the Plasmodium falciparum crt (Pfcrt), Pfmdr1, and Pfmrp genes were not significantly associated with quinine (QN) 50% inhibitory concentrations (IC(50)s) in 23 strains of Plasmodium falciparum. An increased number of DNNND repeats in Pfnhe-1 microsatellite ms4760 was associated
Simon Alex Marshall et al.
Alcoholism, clinical and experimental research, 39(8), 1406-1416 (2015-06-26)
In recent years, much attention has been given to the lack of reproducibility in biomedical research, particularly in preclinical animal studies. This is a problem that also plagues the alcohol research field, particularly in consistent consumption in animal models of
Véronique Parquet et al.
Antimicrobial agents and chemotherapy, 53(6), 2248-2252 (2009-03-25)
Atorvastatin (AVA) is a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. AVA exposure resulted in the reduced in vitro growth of 22 Plasmodium falciparum strains, with the 50% inhibitory concentrations (IC(50)s) ranging from 2.5 microM to 10.8 microM. A significant positive correlation
Matthew L Beckman et al.
Neurochemistry international, 73, 98-106 (2013-10-29)
The serotonin (5-HT) transporter (SERT) is an integral membrane protein that functions to reuptake 5-HT released into the synapse following neurotransmission. This role serves an important regulatory mechanism in neuronal homeostasis. Previous studies have demonstrated that several clinically important antimalarial
Annelies Grimonprez et al.
Brain stimulation, 8(1), 13-20 (2014-12-03)
Depression is the most common psychiatric comorbidity in epilepsy patients. The lack of success with current pharmacological interventions for this patient population, highlights the importance of optimizing non-pharmacological neuromodulatory treatments such as vagus nerve stimulation (VNS). Studies on the antidepressant
Artesunate v. quinine for severe malaria.
P Naidoo et al.
South African medical journal = Suid-Afrikaanse tydskrif vir geneeskunde, 103(5), 274-274 (2013-08-24)
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