Search results for "ECL"

showing 10 items of 1262 documents

Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Anti-HIV activity23-diaryl-13-thiazolidin-4-oneAnti-HIV AgentsCell SurvivalT-LymphocytesDrug Evaluation PreclinicalPharmaceutical SciencePharmacologyVirus ReplicationStructure-Activity RelationshipDrug DiscoveryStructure–activity relationshipHumansCytotoxicityCell survivalAnti hiv activityMolecular StructureAnti hivChemistryvirus diseasesSettore CHIM/08 - Chimica FarmaceuticaReverse transcriptaseIn vitroThiazolesViral replicationHIV-2HIV-1NNRTIsReverse Transcriptase Inhibitors
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Effect of selected triterpenoids on chronic dermal inflammation.

1997

The activity of four natural triterpenoids on a 12-O-tetradecanoylphorbol-13-acetate multiple-dose model of skin chronic inflammation was studied. Erythrodiol and ursolic acid were significantly effective. The most important features concerning structure-activity relationship and previous data on the effect of these triterpenoids on other inflammatory conditions are discussed.

Anti-Inflammatory AgentsDrug Evaluation PreclinicalInflammationPharmacologyDermatitis ContactDexamethasonechemistry.chemical_compoundMiceTriterpenoidDermisUrsolic acidTriterpeneEdemamedicineAnimalsOleanolic AcidBetulinic AcidDexamethasonePharmacologychemistry.chemical_classificationintegumentary systembusiness.industryTriterpenesmedicine.anatomical_structurechemistryImmunologyTetradecanoylphorbol AcetateFemalemedicine.symptombusinessPentacyclic Triterpenesmedicine.drugEuropean journal of pharmacology
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DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.

2019

Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, …

AntifungalCancer chemotherapymedicine.drug_classDrug Evaluation Preclinicaldihydrofolate reductase (DHFR) enzymePharmaceutical ScienceAntineoplastic AgentsComputational biologyReview01 natural scienceshybrid compoundsAnalytical Chemistrylcsh:QD241-44103 medical and health sciencesStructure-Activity RelationshipFolic Acidlcsh:Organic chemistryheterocyclic compoundsNeoplasmsDihydrofolate reductaseparasitic diseasesDrug DiscoverymedicineAnimalsHumansPhysical and Theoretical Chemistry030304 developmental biology0303 health sciencesHeterocyclic compoundbiology010405 organic chemistryDrug discoveryOrganic ChemistryDHFR inhibitors as anticancer agentSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesDHFR drug discoveryTetrahydrofolate DehydrogenaseMechanism of actionChemistry (miscellaneous)Settore CHIM/03 - Chimica Generale E InorganicaDHFR inhibitors as anticancer agentsbiology.proteinMolecular MedicineFolic Acid Antagonistsmedicine.symptomMolecules (Basel, Switzerland)
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Regression Modeling of the Antioxidant-to-Nephroprotective Relation Shows the Pivotal Role of Oxidative Stress in Cisplatin Nephrotoxicity

2021

The clinical utility of the chemotherapeutic drug cisplatin is significantly limited by its nephrotoxicity, which is characterized by electrolytic disorders, glomerular filtration rate decline, and azotemia. These alterations are consequences of a primary tubulopathy causing injury to proximal and distal epithelial cells, and thus tubular dysfunction. Oxidative stress plays a role in cisplatin nephrotoxicity and cytotoxicity, but its relative contribution to overall toxicity remains unknown. We studied the relation between the degree of oxidative reduction (provided by antioxidant treatment) and the extent of nephrotoxicity amelioration (i.e., nephroprotection) by means of a regression anal…

AntioxidantPhysiologymedicine.medical_treatmentClinical BiochemistrycisplatinOxidative phosphorylationRM1-950Pharmacologymedicine.disease_causeBiochemistryArticleNephrotoxicitypreventionpreclinicalMedicineMolecular BiologyCisplatinlinear fitbusiness.industrynephrotoxicityCell Biologymedicine.diseaseantioxidantsErythropoietinToxicityAzotemiaTherapeutics. PharmacologybusinessOxidative stressmedicine.drugAntioxidants
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Gender-related effect of clinical and genetic variables on the cognitive impairment in multiple sclerosis

2004

BACKGROUND: Cognitive impairment may occur at any time during the course of multiple sclerosis (MS), and it is often a major cause of disability in patients with the disease. The APOE-epsilon4 allele is the major known genetic risk factor for late onset familial and sporadic Alzheimer's Disease (AD), and it seems to be implicated in cognitive decline in normal elderly persons. OBJECTIVE: To investigate the clinical and genetic variables that can be associated with the cognitive decline in patients with MS. METHODS: Five-hundred and three patients with clinically definite MS underwent a battery of neuropsychological tests and, according to the number of failed tests, were divided into cognit…

Apolipoprotein EAdultMalemedicine.medical_specialtyPediatricsNeurologyMultiple SclerosisMessengerLate onsetDiseaseNeuropsychological TestsApolipoproteins EmedicineOdds RatioHumansRNA MessengerCognitive declineAllelePsychiatrycognitive impairmentAPOE; Cognitive impairment; Multiple sclerosisAnalysis of VarianceSex CharacteristicsChi-Square DistributionReverse Transcriptase Polymerase Chain ReactionMultiple sclerosisCognitive disorderGenetic VariationMiddle Agedmedicine.diseasemultiple sclerosis cognitive impairment gender geneticNeurologyGenetic Variation; Odds Ratio; Analysis of Variance; Sex Characteristics; Chi-Square Distribution; Humans; Apolipoproteins E; Reverse Transcriptase Polymerase Chain Reaction; Cognition Disorders; RNA Messenger; Multiple Sclerosis; Adult; Middle Aged; Neuropsychological Tests; Female; MaleRNAFemaleSettore MED/26 - NeurologiaNeurology (clinical)Psychologymultiple sclerosis · cognitive impairment · APOECognition DisordersAPOE
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Apolipoprotein E polymorphism is associated with both senile plaque load and Alzheimer-type neurofibrillary tangle formation.

1996

Recent work provided evidence that the apolipoprotein (apo) E polymorphism is associated with late-onset sporadic Alzheimer's disease. The major histological hallmarks of Alzheimer's disease are the extraneuronal deposition of A4/beta-amyloid and the intraneuronal formation of neurofibrillary tangles, the latter correlating strongly with the psychometric status. We examined the relationship between the apo E polymorphism and Alzheimer's disease-related histological changes using a staging system which accounts for the progression of the disease over time and correlates well with the cognitive decline ante mortem. We observed a significant positive correlation between both neurofibrillary ch…

Apolipoprotein EPathologymedicine.medical_specialtyAgingApolipoprotein BGenotypeDiseaseGeneral Biochemistry Genetics and Molecular BiologyApolipoproteins EHistory and Philosophy of ScienceAlzheimer DiseaseMedicineHumansSenile plaquesAlleleCognitive declineApolipoprotein e polymorphismAllelesPolymorphism Geneticbiologybusiness.industryGeneral NeuroscienceBrainNeurofibrillary tangleNeurofibrillary TanglesMiddle Agedmedicine.diseasebiology.proteinRegression AnalysisbusinessAnnals of the New York Academy of Sciences
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Apolipoprotein E polymorphism influences not only cerebral senile plaque load but also Alzheimer-type neurofibrillary tangle formation.

1995

Only recently, evidence was provided that apolipoprotein E allele epsilon 4 located on Chromosome 19 is associated with late onset (i.e. senile) sporadic Alzheimer's disease. Histologically, Alzheimer's disease is associated with intraneuronal neurofibrillary changes and extraneuronal A4/beta-amyloid deposition. We set out with a histological staging system which considers the gradual development of Alzheimer's disease-related histological changes over time and correlates highly with the cognitive decline ante mortem. Our analysis revealed that both the mean stage for A4/beta-amyloid deposits and the mean stage for neurofibrillary tangles get significantly shifted upwards in epsilon 4-carri…

Apolipoprotein EPathologymedicine.medical_specialtyGenotypeLate onsetBiologyCentral nervous system diseaseDegenerative diseaseApolipoproteins EAlzheimer DiseasemedicineHumansSenile plaquesCognitive declineAllelesAgedAged 80 and overAmyloid beta-PeptidesPolymorphism GeneticGeneral NeuroscienceAge FactorsBrainNeurofibrillary tangleNeurofibrillary TanglesMiddle Agedmedicine.diseaseRegression AnalysisAlzheimer's diseaseChromosomes Human Pair 19Neuroscience
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NOTES ON A STATUE FROM THE COLLECTIONS OF THE NATIONAL MUSEUM OF UNION FROM ALBA IULIA

2016

This study proposes to re-evaluate a marble statue from the old collections of the National Museum of Union Alba Iulia. It was discovered by A. Cserni during excavations carried out at the Palace of the Governors of Roman Dacia, in 1898. It has been repeatedly published by Á. Hekler and Al. Diaconescu. While the latter author established dating and iconographic prototype of the statue, we believe that further details as discovery place and context, depiction, iconographic attribution and role of this work of art can be offered. Presence of a follower at the feet of the divinity, more precisely the right foot of a character – child, conveys us the idea of depiction of Eros, god of love. Usua…

ArcheologyHistorybusiness.industryapulum eros goddess marble statue prototype venus.Art historyContext (language use)Character (symbol)Representation (arts)Ancient historyD51-90PoliticsArchaeologyDivinityMedicineDepictionStatueClassicsbusinessCC1-960EclecticismJOURNAL OF ANCIENT HISTORY AND ARCHAEOLOGY
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‘Adaptive cycles’ and climate fluctuations: a case study from Linear Pottery Culture in western Central Europe

2014

Abstract By applying cycle-based resilience theory the dynamics of the Early Neolithic west-central European Linear Pottery Culture (LBK) are investigated. These are interpreted as resulting from a combination of internal socio-economic processes as well as external environmental parameters. Resilience theory is helpful in understanding periods of increased vulnerability and inherent trends to social complexity. Cycles and threshold levels also help to understand why societies experience periods of increasing fragility and subsequent decline. Results are based on the correlation of a typology and dendrochronology-based archaeological chronology for western LBK and various palaeoclimatic pro…

Archeologyeducation.field_of_studyEcologyArchaeological recordPopulationSocial complexity15. Life on landPopulation declineGeography13. Climate actionPeriod (geology)Population growthPhysical geographyPotteryeducationChronologyJournal of Archaeological Science
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Señor. El Cabildo de la Santa Iglesia Metropolitana de la Ciudad de Lima, en Sede-vacante ... dice: Que por el Testimonio de Autos remitido à V. Ma…

1731

Com a tít. el començament del text Caplletres ornades Sign.: A4 Reclams

Armendáriz José Marqués de Castel-Fuerte Virrey del Perú Obres anteriors a 1800Armendáriz José Marqués de Castel-Fuerte Virrey del Perú Obres anteriors al 1800Immunitat eclesiàstica Obres anteriors a 1800Franciscans Lima (Perú) 1731 Obres anteriors al 1800Franciscans Lima (Perú) 1731 Obres anteriors a 1800Catedral de Lima 1731 Obres anteriors a 1800Catedral de Lima 1731 Obres anteriors al 1800Immunitat eclesiàstica Obres anteriors al 1800
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