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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells
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Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: Discovery of potent S1P1 receptor agonists
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Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors
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3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists
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Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase
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Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1
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Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
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Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles
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BCUT descriptors to predicting affinity toward A3 adenosine receptors
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Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist
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Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
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Design, synthesis, and structure–activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis
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SAR of psilocybin analogs: Discovery of a selective 5-HT2C agonist
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Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists
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Screening of active compounds as neuromedin U2 receptor agonist from natural products
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An efficient synthesis of aryloxyphenyl cyclopropyl methanones: a new class of anti-mycobacterial agents
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Hepatitis C virus NS3-4A serine protease inhibitors: Use of a P2–P1 cyclopropyl alanine combination for improved potency
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Facile synthesis and PET imaging of a novel potential heart acetylcholinesterase tracer N-[11C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2′,2′-diphenylpropionoxymethyl)pyridinium
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Synthesis and antibacterial activity of N-(5-benzylthio-1,3,4-thiadiazol-2-yl) and N-(5-benzylsulfonyl-1,3,4-thiadiazol-2-yl)piperazinyl quinolone derivatives
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Synthesis and cytotoxic activity of platinum complex immobilized by branched polyethylene glycol
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Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors
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Synthesis and evaluation of anti-HIV activity of isatin β-thiosemicarbazone derivatives
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Design and synthesis of phthalimide-type histone deacetylase inhibitors
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Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors
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Synthesis and biological evaluation of novel (l)-α-amino acid methyl ester, heteroalkyl, and aryl substituted 1,4-naphthoquinone derivatives as antifungal and antibacterial agents
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A minimum thickness gate valve with integrated ion optics for mass spectrometry
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A Personal Retrospective of the Early Years
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Directory of Corporate Members
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A Study on Mass Spectrometry of Methylated [60] Fullerenes Using the “In-beam” Electron Impact Technique
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Ion Funnels for the Masses: Experiments and Simulations with a Simplified Ion Funnel
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Identification of a new source of interference leached from polypropylene tubes in mass-selective analysis
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Trap for MAbs: Characterization of intact monoclonal antibodies using reversed-phase HPLC on-line with ion-trap mass spectrometry
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ZoomQuant: An application for the quantitation of stable isotope labeled peptides
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Evidence for Unfolding and Refolding of Gas-Phase Cytochrome c Ions in a Paul Trap
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Porous Anodic Alumina Membrane as a Sample Support for MALDI-TOF MS Analysis of Salt-Containing Proteins
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Immobilization of Aminophenylboronic Acid on Magnetic Beads for the Direct Determination of Glycoproteins by Matrix Assisted Laser Desorption Ionization Mass Spectrometry
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MALDI Mass Spectrometry Analysis of High Molecular Weight Proteins from Whole Bacterial Cells: Pretreatment of Samples with Surfactants
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Characterization of an N-acylated glucagon-like peptide-1 derivative by electron capture dissociation
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Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity
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The pathway to commercialization for nanomedicine
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Drug-loaded, magnetic, hollow silica nanocomposites for nanomedicine
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Intracellular analysis of Saccharomyces cerevisiae using CLSM after ultrasonic treatments
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Influence of nanoscale surface roughness on neural cell attachment on silicon
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A review: Integrin αvβ3-targeted molecular imaging and therapy in angiogenesis
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Will the nanomedicine “patent land grab” thwart commercialization?
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Stability of C60 chains: molecular dynamics simulations
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Simulating adsorption of n-heptane in the Pt/Al2O3 model: Influence of platinum
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N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities
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Structure–activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads
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Hydantoin derivative formation from oxidation of 7,8-dihydro-8-oxo-2′-deoxyguanosine (8-oxodG) and incorporation of 14C-labeled 8-oxodG into the DNA of human breast cancer cells
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First asymmetric aminohydroxylation of acrylamides
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Enzymatic kinetic resolution of tropic acid
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A new strategy for the synthesis of hydroxylated pyrrolizidinic alkaloids by highly stereoselective indium-mediated allylation of pyrrolidinic aldehydes
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The asymmetric Michael-type alkylation of chiral β-enamino esters: critical role of a benzyl ester group in the racemization of adducts
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High enantio- and diastereoselective induction of BINOL- and TADDOL-modified vinyloxy ethoxides in C-C coupling reactions with aldehydes
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A convenient synthesis of the enantiomerically pure β-blocker (S)-betaxolol using hydrolytic kinetic resolution
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First enantiopure calix[6]aza-cryptand: synthesis and chiral recognition properties towards neutral molecules
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An efficient enzyme-catalyzed kinetic resolution: large-scale preparation of an enantiomerically pure indole-ethyl ester derivative, a key component for the synthesis of a prostaglandin D2 receptor antagonist, an anti-allergic rhinitis drug candidate
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Memory of chirality trapping of low inversion barrier 1,4-benzodiazepin-2-one enolates
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The bidentate complexes of (R,R)- and meso-α,α′-bis(trifluoromethyl)-9,10-anthracenedimethanol with cis-1-amino-2-indanol
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An asymmetric aminohydroxylation route to (+)-l-733,060
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Microbial oxidation/amidation of benzhydrylsulfanyl acetic acid. Synthesis of (+)-modafinil
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Synthesis of sterically controlled chiral β-amino alcohols and their application to the catalytic asymmetric sulfoxidation of sulfides
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Improved preparation of β-hydroxy-α-amino acids: direct formation of sulfates by sulfuryl chloride
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Cumulative author index
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Stereodifferentiation in the fluorescence of naproxen–arginine salts in the solid state
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Thioether–phosphinite and diphosphinite ligands derived from d-xylose for the copper-catalyzed asymmetric 1,4-addition to 2-cyclohexenone
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Preparation of (S)-mandelic acids by enantioselective degradation of racemates with a new isolate Pseudomonas putida ECU1009
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Application of the N-hydroxymethyl group to the stereoselective synthesis of (3S,4S)-3-aminodeoxystatine derivatives
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A method to greatly improve the enantioselectivity of lipase-catalyzed hydrolysis using sodium dodecyl sulfate (SDS) as an additive
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Synthesis of 3 or 3,3′-substituted BINOL ligands and their application in the asymmetric addition of diethylzinc to aromatic aldehydes
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Enantiopure cycloheptenones from (R)-(−)-carvone: intermediates for perhydroazulene terpenoids
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A stereoselective synthesis of (2S,4R)-δ-hydroxyleucine methyl ester: a component of cyclomarin A
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Preliminary studies on the synthesis of rancinamycins from nitrosugars: first total synthesis of (3S,4S,5S,6R)-5-benzyloxy-6-hydroxy-3,4-(isopropylidendioxy)-cyclohex-1-enecarbaldehyde
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A new and effective method for providing optically active monosubstituted malononitriles: selective reduction of α,β-unsaturated dinitriles catalyzed by copper hydride complexes
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Asymmetric synthesis of 1,4-amino alcohol ligands with a norbornene backbone for use in the asymmetric diethylzinc addition to benzaldehyde
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Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors
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Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
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Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure–activity relationships
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2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV
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Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1
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Asymmetric synthesis of O-benzoyl cyanohydrins by reaction of aldehydes with benzoyl cyanide catalysed by BINOLAM–Ti(IV) complexes
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Preparation of the four stereoisomers of 3-bromo-2-butanol or their acetates via lipase-catalysed resolutions of the racemates derived from dl- or meso-2,3-butanediol
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Synthesis of enantiopure cyclobutane amino acids and amino alcohols
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Resolution of non-protein amino acids via Carica papaya lipase-catalyzed enantioselective transesterification
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Highly stereoselective preparation of (3R,4S)-3,4-chromanediol by deracemization of (±)-3-hydroxy-4-chromanone by Trichosporon cutaneum
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Influence on the enantioselectivity in allylic alkylation of the spacer between the amido group of d-glucosamine and the diphenylphosphino group
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Cumulative author index
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In Situ Structural Characterization of Phosphatidylcholines in Brain Tissue Using MALDI-MS/MS
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A catalytic asymmetric synthesis of 5,5-dimethylproline
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Synthesis, structure, and stereochemistry of the bora derivatives of 1-[(2-hydroxy-1-naphthyl)methyl]proline
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A re-investigation of Modena’s protocol for the asymmetric oxidation of prochiral sulfides
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Chemoenzymatic synthesis of N-Boc protected (2S,3R)-3-hydroxy-3-methylproline
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Short enantioselective synthesis of sedridines, ethylnorlobelols and coniine via reagent-based differentiation
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Stereo- and regioselective construction of vicinal stereogenic quaternary carbon atoms: enantiospecific approach to cyperanes
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Synthesis of (S)-(−)- and (R)-(+)-O-methylbharatamine using a diastereoselective Pomeranz–Fritsch–Bobbitt methodology
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Fluorescent probes of d-(+)-gluconic acid δ-lactone based on binary hosts of chiral calix[5]arene
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A simple and practical approach to enantiomerically pure (S)-3-hydroxy-γ-butyrolactone: synthesis of (R)-4-cyano-3-hydroxybutyric acid ethyl ester
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Univocal syntheses of 2- and 3-hydroxymethyl-2,3-dihydro[1,4]dioxino[2,3-b]pyridine enantiomers
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Graphical contents list
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