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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

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Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding
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Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers
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5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa
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Novel β-(imidazol-4-yl)-β-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I
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Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs
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QSAR for anti-RNA-virus activity, synthesis, and assay of anti-RSV carbonucleosides given a unified representation of spectral moments, quadratic, and topologic indices
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Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators
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Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain
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QSAR studies on 1,2-dithiole-3-thiones: modeling of lipophilicity, quinone reductase specific activity, and production of growth hormone
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Identification of a UDP-Gal: GlcNAc-R galactosyltransferase activity in Escherichia coli VW187
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Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
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Studies on synthesis and evaluation of quantitative structure-activity relationship of 5-[(3′-chloro-4′,4′-disubstituted-2-oxoazetidinyl)(N-nitro)amino]-6-hydroxy-3-alkyl/aryl[1,3]azaphospholo[1,5-a]pyridin-1-yl-phosphorus dichlorides
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QSAR study on pKa vis-à-vis physiological activity of sulfonamides: a dominating role of surface tension (inverse steric parameter)
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Preparation and characterization of solid lipid nanoparticles (SLN) made of cacao butter and curdlan
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Fast-dissolving mucoadhesive microparticulate delivery system containing piroxicam
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Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug
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Effects of miltefosine on membrane permeability and accumulation of [99mTc]-hexakis-2-methoxyisobutyl isonitrile, 2-[18F]fluoro-2-deoxy-d-glucose, daunorubucin and rhodamine123 in multidrug-resistant and sensitive cells
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Preparation and evaluation of release characteristics of 3TabGum, a novel chewing device
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Instructions to Authors
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Characterization of the rotating dialysis cell as an in vitro model potentially useful for simulation of the pharmacokinetic fate of intra-articularly administered drugs
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Targeting liposomes with protein drugs to the blood-brain barrier in vitro
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Acid-base properties of selected flavonoid glycosides
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AZD3582 increases heme oxygenase-1 expression and antioxidant activity in vascular endothelial and gastric mucosal cells
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Effect of staurosporine on N-glycosylation and cell adhesion to fibronectin of SW480 human colorectal adenocarcinoma cells
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Nanoparticle uptake by the oral route: Fulfilling its potential?
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Overactive bladder: Targeting prostaglandins in sensory pathways
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AMP-activated protein kinase and malonyl-CoA: Targets for treating insulin resistance?
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Dipeptidyl peptidase IV inhibitors for type 2 diabetes and metabolic syndrome
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Therapeutic strategies for targeting PTP1B in diabetes
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LXR: A nuclear receptor target for cardiovascular disease?
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Challenges and opportunities associated with targeting estrogen receptors in treating hypertension and cardiovascular disease
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Peroxisome Proliferator-Activated Receptor β/δ: A novel target for the reduction of atherosclerosis
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Targeting the vascular RhoA-Rho-kinase signaling pathway in hypertension
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Preclinical in vitro screening assays for drug-like properties
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Accelerating lead development by microwave-enhanced medicinal chemistry
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Genome scale cytometry: High content analysis for high throughput RNAi phenotype profiling
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Nonviral gene delivery systems: From simple transfection agents to artificial viruses
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Salt formation in solid dispersions consisting of polyacrylic acid as a carrier and three basic model compounds resulting in very high glass transition temperatures and constant dissolution properties upon storage
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Buccal drug delivery: A challenge already won?
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New poly(lactic-co-glycolic acid) derivatives: Modular polymers with tailored properties
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Mass spectrometry-based methods for biomarker detection and analysis
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Protein pathway analysis in Clinical Proteomics using protein microarrays
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Integrating disease knowledge and technology to deliver protein targets and biomarkers into drug discovery projects
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Affinity assays for decrypting protein targets of unknown function
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5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization
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QSAR study on the antibacterial activity of some sulfa drugs: building blockers of Mannich bases
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Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones
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Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists
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Unified Markov thermodynamics based on stochastic forms to classify drugs considering molecular structure, partition system, and biological species:
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QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools
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GETAWAY descriptors to predicting A2A adenosine receptors agonists
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Pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones
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Iminosugars as glycosyltransferase inhibitors: synthesis of polyhydroxypyrrolidines and their evaluation on chitin synthase activity
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QSAR analysis of thiazole benzenesulfonamide substituted 3-pyridylethanolamines as β3-adrenergic receptor agonist
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Hologram quantitative structure–activity relationships for a series of farnesoid X receptor activators
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Carbonic anhydrase inhibitors: Novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX
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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines
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Synthesis and SAR of novel oxazolidinones: Discovery of ranbezolid
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Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure–activity relationships of the 7- and 5-, 6-, 8-positions
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Synthesis and bladder smooth muscle relaxing properties of substituted 3-amino-4-aryl-(and aralkyl-)cyclobut-3-ene-1,2-diones
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Synthesis and structure–activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1)
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Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors
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Structural characterization and antimicrobial activity of 1,3-bis(2-benzimidazyl)-2-thiapropane ligand and its Pd(II) and Zn(II) halide complexes
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Oral delivery of G protein-coupled receptor modulators: An explanation for the observed class difference
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The characterization of a novel rigid nicotine analog with α7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion
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Carbonic anhydrase inhibitors: Design of thioureido sulfonamides with potent isozyme II and XII inhibitory properties and intraocular pressure lowering activity in a rabbit model of glaucoma
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Proteins QSAR with Markov average electrostatic potentials
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Analysis of structure–activity relationships for the ‘A-region’ of N-(4-t-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists
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Trichloroacetaldehyde modified oligonucleotides
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Molecular recognition of 15-deoxy-Δ12,14-prostaglandin J2 by nuclear factor-kappa B and other cellular proteins
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Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid
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Antioxidant and antiproliferative activity of curcumin semicarbazone
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Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs
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Surfing the piperazine core of tricyclic farnesyltransferase inhibitors
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Synthesis and antifungal activity of 2/3-arylthio- and 2,3-bis(arylthio)-5-hydroxy-/5-methoxy-1,4-naphthoquinones
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Synthesis and biological evaluation of new N-substituted-N′-(3,5-di/1,3,5-trimethylpyrazole-4-yl)thiourea/urea derivatives
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Effects of RM-β-CD on sublingual bioavailability of Δ9-tetrahydrocannabinol in rabbits
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Development of a single unit extended release formulation for ZK 811 752, a weakly basic drug
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Intranasal delivery of recombinant human growth hormone (somatropin) in sheep using chitosan-based powder formulations
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Kinetic values for mechanism-based enzyme inhibition: Assessing the bias introduced by the conventional experimental protocol
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Disorder and dissolution enhancement: Deposition of ibuprofen on to insoluble polymers
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Drug permeability in 16HBE14o- airway cell layers correlates with absorption from the isolated perfused rat lung
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Why optimize cancer drugs for ADMET?
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Parkinson's disease as a disorder of the aging
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Synthesis, in vitro cytotoxic and antiviral activity of cis-[Pt(R(-) and S(+)-2-α-hydroxybenzylbenzimidazole)2Cl2] complexes
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NO-donors, part 9 [1]: diazeniumdiolates inhibit human platelet aggregation and induce a transient vasodilatation of porcine pulmonary arteries in accordance with the NO-releasing rates
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HIV protease inhibitors: synthesis and activity of N-aryl-N′-hydroxyalkyl hydrazide pseudopeptides
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Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors
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Synthesis and antimicrobial activity of 4-phenyl/cyclohexyl-5-(1-phenoxyethyl)-3-[N-(2-thiazolyl)acetamido]thio-4H-1,2,4-triazole derivatives
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Synthesis, physicochemical and in vitro pharmacological investigation of new platinum (II) complexes with some cycloalkanespiro-5′-hydantoins
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Synthesis and study of antibacterial and antifungal activities of novel 8-methyl-7,9-diaryl-1,2,4,8-tetraazaspiro[4.5]decan-3-thiones
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The synthesis and antimicrobial activity of some new methyl N-arylthiocarbamates, dimethyl N-aryldithiocarbonimidates and 2-arylamino-2-imidazolines
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Epoxide-containing side chains enhance antiproliferative activity of paullones
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An unexpected amide bond cleavage: poly (ethylene glycol) transport forms of vancomycin. 2
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New thiophene analogues of kenpaullone: synthesis and biological evaluation in breast cancer cells
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Synthesis and anticancer evaluation of certain 4-anilinofuro[2,3-b]quinoline and 4-anilinofuro[3,2-c]quinoline derivatives
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Synthesis and antimalarial activity of E-2-quinolinylbenzocycloalcanones
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Synthesis and antimicrobial study of novel heterocyclic compounds from hydroxybenzophenones
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Synthesis and structure-activity relationships of mono- and dialkyl-substituted oxaliplatin derivatives
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