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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Highly enantioselective sequential Claisen-Ireland/metathesis: synthesis of cycloalkenes bearing two contiguous highly functionalized asymmetric centres
Fulltext Access 15 Pages 2005
Synthetic disaccharide analogs as potential substrates and inhibitors of a mycobacterial polyprenol monophosphomannose-dependent α-(1→6)-mannosyltransferase
Fulltext Access 15 Pages 2005
A novel class of sodium/calcium exchanger inhibitor: design, synthesis, and structure–activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives
Fulltext Access 15 Pages 2005
Novel 3-amino-2-hydroxy acids containing protease inhibitors. Part 1: Synthesis and kinetic characterization as aminopeptidase P inhibitors
Fulltext Access 15 Pages 2005
From glycoside hydrolases to thioglycoligases: the synthesis of thioglycosides
Fulltext Access 15 Pages 2005
2,9-Disubstituted-N6-(arylcarbamoyl)-8-azaadenines as new selective A3 adenosine receptor antagonists: Synthesis, biochemical and molecular modelling studies
Fulltext Access 15 Pages 2005
Pyrazolopyridine antiherpetics: SAR of C2′ and C7 amine substituents
Fulltext Access 15 Pages 2005
Anomeric α-azido acid (2-azido-2-deoxy-hept-2-ulopyranosonic acid) derivatives en route to peptides incorporating sugar amino acids
Fulltext Access 15 Pages 2005
Disarming, non-participating 2-O-protecting groups in manno- and rhamnopyranosylation: scope and limitations of sulfonates, vinylogous esters, phosphates, cyanates, and nitrates
Fulltext Access 15 Pages 2005
Chiral catalysts in the stereoselective synthesis of pyrrolidine derivatives via metallo-azomethine ylides
Fulltext Access 15 Pages 2005
Dolastatin 11 conformations, analogues and pharmacophore
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Two novel series of allocolchicinoids with modified seven membered B-rings: design, synthesis, inhibition of tubulin assembly and cytotoxicity
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Semiempirical MO approach to the mechanism of the NIS-mediated nucleophilic addition to glycals: multicomponent intermediates as models to tackle reactivity in organic chemistry
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Structure–activity relationships and molecular modelling of 5-arylidene-2,4-thiazolidinediones active as aldose reductase inhibitors
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Pathways of Peptide Ion Fragmentation Induced by Vacuum Ultraviolet Light
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A physically interpretable quantum-theoretic QSAR for some carbonic anhydrase inhibitors with diverse aromatic rings, obtained by a new QSAR procedure
Fulltext Access 15 Pages 2005
Formation of [b(n−1) + OH + H]+ Ion Structural Analogs by Solution-Phase Chemistry
Fulltext Access 15 Pages 2005
Ion Excitation in a Linear Quadrupole Ion Trap with an Added Octopole Field
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Synthesis, solution structure, and bioactivity of six new simplified analogues of the natural cyclodepsipeptide jaspamide
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C2-Symmetric nitroxides and their potential as enantioselective oxidants
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Matched and mismatched pairings in B-secotaxane construction: a structure elucidation study
Fulltext Access 15 Pages 2005
The aldol–annulation–fragmentation strategy toward the taxoid diterpene framework revisited. Instructive failures in the chemistry of medium ring containing systems
Fulltext Access 15 Pages 2005
Synthesis and pharmacological evaluation of 4H-1,4-benzothiazine-2-carbonitrile 1,1-dioxide and N-(2-cyanomethylsulfonylphenyl)acylamide derivatives as potential activators of ATP sensitive potassium channels
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Inhibitory activity of polyhydroxycarboxylate chelators against recombinant NF-κB p50 protein-DNA binding
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Discovery of an N-(2-aminopyridin-4-ylmethyl)nicotinamide derivative: a potent and orally bioavailable NCX inhibitor
Fulltext Access 15 Pages 2005
Synthesis of 4-(1-oxo-isoindoline) and 4-(5,6-dimethoxy-1-oxo-isoindoline)-substituted phenoxypropanolamines and their β1-, β2-adrenergic receptor binding studies
Fulltext Access 15 Pages 2005
C3′-cis-Substituted carboxycyclopropyl glycines as metabotropic glutamate 2/3 receptor agonists: Synthesis and SAR studies
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Molecular modeling, design, synthesis, and biological evaluation of novel 3′,4′-dicamphanoyl-(+)-cis-khellactone (DCK) analogs as potent anti-HIV agents
Fulltext Access 15 Pages 2005
New high affinity H3 receptor agonists without a basic side chain
Fulltext Access 15 Pages 2005
Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues
Fulltext Access 15 Pages 2005
Synthesis of 17β-estradiol-linked platinum(II) complexes and their cytocidal activity on estrogen-dependent and -independent breast tumor cells
Fulltext Access 15 Pages 2005
Polymorphism of paracetamol: Relative stabilities of the monoclinic and orthorhombic phases inferred from topological pressure‐temperature and temperature‐volume phase diagrams
Fulltext Access 16 Pages 2005
Reactivity of substituted and unsubstituted diphenyephosphonium diylides towards carbonic anhydride derivatives.
Fulltext Access 16 Pages 2005
Comparison of a Miniaturized Shake-Flask Solubility Method with Automated Potentiometric Acid/Base Titrations and Calculated Solubilities
Fulltext Access 16 Pages 2005
Quantitative Structure-Pharmacokinetic Relationships for Drug Distribution Properties by Using General Regression Neural Network
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Stability of 5-aminolevulinic acid in novel non-aqueous gel and patch-type systems intended for topical application
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Hybrid films from blends of chitosan and egg phosphatidylcholine for localized delivery of paclitaxel
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Differential binding properties of [3H]dextrorphan and [3H]MK-801 in heterologously expressed NMDA receptors
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Interactions between CAP70 and actinfilin are important for integrity of actin cytoskeleton structures in neurons
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Asymmetric synthetic study of macrolactin analogues
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Plasticity-specific phosphorylation of CaMKII, MAP-kinases and CREB during late-LTP in rat hippocampal slices in vitro
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Cholinergic modulation of the spatiotemporal pattern of hippocampal activity in vitro
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Morphine alters the selective association between mu-opioid receptors and specific RGS proteins in mouse periaqueductal gray matter
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A mild and practical copper catalyzed amination of halothiophenes
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Imaging addiction with PET: is insight in sight?
Fulltext Access 16 Pages 2005
Fragmentation of Negative Ions from Carbohydrates: Part 2. Fragmentation of High-Mannose N-Linked Glycans
Fulltext Access 16 Pages 2005
Tandem Mobility Mass Spectrometry Study of Electrosprayed Tetraheptyl Ammonium Bromide Clusters
Fulltext Access 16 Pages 2005
Assigning product ions from complex MS/MS spectra: The importance of mass uncertainty and resolving power
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Effects of Solvent Flow, Dopant Flow, and Lamp Current on Dopant-Assisted Atmospheric Pressure Photoionization (DA-APPI) for LC-MS. Ionizationvia Proton Transfer
Fulltext Access 16 Pages 2005
An interdisciplinary approach to certain fundamental issues in the fields of physics and biology: towards a unified theory
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1-Amino-1-ferrocenyl-2-methyl-2-propanol: a case study on the conformational control of asymmetric induction
Fulltext Access 16 Pages 2005
Atom, atom-type and total molecular linear indices as a promising approach for bioorganic and medicinal chemistry: theoretical and experimental assessment of a novel method for virtual screening and rational design of new lead anthelmintic
Fulltext Access 16 Pages 2005
Chemical-biological interactions in human
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Synthesis and pharmacological evaluation of glycine-modified analogues of the neuroprotective agent glycyl-l-prolyl-l-glutamic acid (GPE)
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Aza-Wittig reaction of fluoroalkylated N-vinylic phosphazenes with carbonyl compounds. Usefulness of 2-azadienes for the preparation of fluoroalkyl pyridine derivatives
Fulltext Access 16 Pages 2005
Altering protein specificity: techniques and applications
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Novel fluoropeptidomimetics: synthesis, stability studies and protease inhibition
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Effect of change in nucleoside structure on the activation and antiviral activity of phosphoramidate derivatives
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Development of α-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease
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Synthesis of novel substituted 2-phenylpyrazolopyridines with potent activity against herpesviruses
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Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives
Fulltext Access 16 Pages 2005
5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure–activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors
Fulltext Access 16 Pages 2005
Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists
Fulltext Access 16 Pages 2005
Studies on the Mechanism of Aspartic Acid Cleavage and Glutamine Deamidation in the Acidic Degradation of Glucagon
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Potent, selective, and orally bioavailable matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis
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Deamidation of model β-turn cyclic peptides in the solid state
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Diclofenac Salts. III. Alkaline and Earth Alkaline Salts
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Tunable phosphinite, phosphite and phosphoramidite ligands for the asymmetric hydrovinylation reactions
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Reactions of guaiazulene with methyl terephthalaldehydate and 2-hydroxy- and 4-hydroxybenzaldehydes in methanol in the presence of hexafluorophosphoric acid: comparative studies on molecular structures and spectroscopic, chemical and electrochemical prope
Fulltext Access 16 Pages 2005
Regioselective reactivity of some 5,7-dimethoxyindoles
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Synthesis of porphyrazine-octaamine, hexamine and diamine derivatives
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Synthesis of granulatimide bis-imide analogues
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Cycloaddition reactions on activated exo-glycals
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Synthesis of functionalized α-amino-phosphine oxides and -phosphonates by addition of amines and aminoesters to 4-phosphinyl- and 4-phosphonyl-1,2-diaza-1,3-butadienes
Fulltext Access 16 Pages 2005
XYZH systems as potential 1,3-dipoles. Part 62:1 1,3-Dipolar cycloaddition reactions of metallo-azomethine ylides derived from α-iminophosphonates
Fulltext Access 16 Pages 2005
Synthetic studies on 3-arylquinazolin-4-ones: intramolecular nucleophilic aromatic substitution reaction of 2-carboxamido-3-arylquinazolin-4-ones and its application to the synthesis of secondary aryl amines
Fulltext Access 16 Pages 2005
Synthesis of l-arabinopyranose containing hederagenin saponins
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Oxidative addition of N-halosuccinimides to palladium(0): the discovery of neutral palladium(II) imidate complexes, which enhance Stille coupling of allylic and benzylic halides
Fulltext Access 16 Pages 2005
Dynamic resolution of N-alkyl-2-lithiopyrrolidines with the chiral ligand (−)-sparteine
Fulltext Access 16 Pages 2005
Rigid backbone 1,8-anthracene-linked bis-oxazolines (AnBOXes): design, synthesis, application and characteristics in catalytic asymmetric aziridination
Fulltext Access 17 Pages 2005
Novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I (hDPPI)
Fulltext Access 17 Pages 2005
Novel 5-substituted, 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors with antiangiogenic and antitumor activity
Fulltext Access 17 Pages 2005
Trichosporon beigelli esterase (TBE): a versatile esterase for the resolution of economically important racemates
Fulltext Access 17 Pages 2005
Synthesis of novel chiral hydrobenzoin mono-tert-butyl ethers derived from m-hydrobenzoin and their application as chiral auxiliaries in the diastereoselective reduction of α-keto esters
Fulltext Access 17 Pages 2005
Development of 3,4-dihydro-2H-benzo[1,4]oxazine derivatives as dual thromboxane A2 receptor antagonists and prostacyclin receptor agonists
Fulltext Access 17 Pages 2005
Novel matrix metalloproteinase inhibitors: Generation of lead compounds by the in silico fragment-based approach
Fulltext Access 17 Pages 2005
Design, synthesis and characterization of a novel class of coumarin-based inhibitors of inducible nitric oxide synthase
Fulltext Access 17 Pages 2005
Ion-Ion and Ion-Molecule Reactions at the Surface of Proteins Produced by Nanospray. Information on the Number of Acidic Residues and Control of the Number of Ionized Acidic and Basic Residues
Fulltext Access 17 Pages 2005
Toward a general mechanism of electron capture dissociation
Fulltext Access 17 Pages 2005
Core-modified porphyrins. Part 4: Steric effects on photophysical and biological properties in vitro
Fulltext Access 17 Pages 2005
Dielectric Studies of Molecular Motions in Amorphous Solid and Ultraviscous Acetaminophen
Fulltext Access 17 Pages 2005
An Evaluation of the Utility of Physiologically Based Models of Pharmacokinetics in Early Drug Discovery
Fulltext Access 17 Pages 2005
A Comparison of the Gas Phase Acidities of Phospholipid Headgroups: Experimental and Computational Studies
Fulltext Access 17 Pages 2005
Caco-2 permeability of weakly basic drugs predicted with the Double-Sink PAMPA pKaflux method
Fulltext Access 17 Pages 2005
RGS-Rz and RGS9-2 proteins control mu-opioid receptor desensitisation in CNS: the role of activated Gαz subunits
Fulltext Access 17 Pages 2005
The dopamine D3 receptor and drug dependence: Effects on reward or beyond?
Fulltext Access 17 Pages 2005
Role of the α subunit in the modulation of GABAA receptors by anabolic androgenic steroids
Fulltext Access 17 Pages 2005
An approach to solvent screening for crystallization of polymorphic pharmaceuticals and fine chemicals
Fulltext Access 17 Pages 2005
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure
Fulltext Access 17 Pages 2005
Table ronde animée par Laurent Broomhead*
Fulltext Access 17 Pages 2005
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