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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Insecticidal activity of proteinous venom from tentacle of jellyfish Rhopilema esculentum Kishinouye
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1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors
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Active site directed inhibitors of replication-specific bacterial DNA polymerases
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Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans
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Pyrenyldiazomethane, a versatile reagent for nucleotide phosphate alkylation
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Synthesis and antifungal activity of noble 5-arylamino- and 6-arylthio-4,7-dioxobenzoselenazoles
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Parallel synthesis of pteridine derivatives as potent inhibitors for hepatitis C virus NS5B RNA-dependent RNA polymerase
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Cleavage at 5-methylcytosine in DNA by photosensitized oxidation with 2-methyl-1,4-naphthoquinone tethered oligodeoxynucleotides
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Truncated azinomycin analogues intercalate into DNA
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Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold
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Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands
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Synthesis of 2-[3,5-substituted pyrazol-1-yl]-4,6-trisubstituted triazine derivatives as antimalarial agents
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Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol
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Design and synthesis of macrocycles active against vancomycin-resistant enterococci (VRE): the interplay between d-Ala-d-Lac binding and hydrophobic effect
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Design, synthesis, and enzymatic property of a sulfur-substituted analogue of trigalacturonic acid
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Solid support synthesis of 6-aryl-2-substituted pyrimidin-4-yl phenols as anti-infective agents
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The synthesis and 16S A-site rRNA recognition of carbohydrate-free aminoglycosides
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The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines
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Solid-phase synthesis and anti-infective activity of a combinatorial library based on the natural product anisomycin
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Contribution of site-specific PEGylation to the dipeptidyl peptidase IV stability of glucose-dependent insulinotropic polypeptide
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1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles
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Controllable selective synthesis of a polymerizable prodrug of cytarabine by enzymatic and chemical methods
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Influence of acid surrogates toward potency of VLA-4 antagonist
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Utilizing the intramolecular Fukuyama–Mitsunobu reaction for a flexible synthesis of novel heterocyclic scaffolds for peptidomimetic drug design
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Synthesis and structure–activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists
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Synthesis of cyclic peptidosulfonamides as scaffolds for MC4 pharmacophoric groups
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Instructions to Authors
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Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme
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Synthesis and SAR of novel 4,5-diarylimidazolines as potent P2X7 receptor antagonists
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Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis
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Pyrimidine containing RSV fusion inhibitors
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IKCa-channel blockers. Part 2: Discovery of cyclohexadienes
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Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors
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(S,E)-N-[1-(3-Heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity
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Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus
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Potent 4-aminopiperidine based antimalarial agents
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Schizophyllan-folate conjugate as a new non-cytotoxic and cancer-targeted antisense carrier
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Structure-antioxidant activity relationships of flavonoids isolated from the resinous exudate of Heliotropium sinuatum
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New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: Synthesis and biological activity
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Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers
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A new ligand binding to G-G mismatch having improved thermal and alkaline stability
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Discovery of a novel, potent and selective human β3-adrenergic receptor agonist
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Instructions to contributors
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Crystallographic determination of stereochemistry of biologically active 2″,3″-dibromo-7-epi-10-deacetylcephalomannine
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DNA topoisomerase I inhibitors from Rinorea anguifera
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1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents
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Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies
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Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors
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Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships
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Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT7 receptor
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A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor
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Synthesis of (1,4)-naphthoquinono-[3,2-c]-1H-pyrazoles and their (1,4)-naphthohydroquinone derivatives as antifungal, antibacterial, and anticancer agents
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Metabolism investigation leading to novel drug design: Orally active prostacyclin mimetics. Part 4
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Synthesis and biological evaluation of novel bisphosphonates with dual activities on bone in vitro
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Novel phomactin analogues as PAF receptor ligands
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6-(2-Phenylethyl)nicotine: A novel nicotinic cholinergic receptor ligand
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Synthesis and antitumor activity of the hexacyclic camptothecin derivatives
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Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists
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Action of a novel pyrrolo[1,2-c][1.3]benzodiazepine on the viability of Jurkat and neuronal/glial cells
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Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as α1-adrenoceptor antagonists
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Cell differentiation inducers derived from thalidomide
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Discovery of non-steroidal mifepristone mimetics: Pyrazoline-based PR antagonists
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Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
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Discovery and synthesis of a novel and selective drug-like P2X1 antagonist
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Investigation of human serum albumin (HSA) binding specificity of certain photosensitizers related to pyropheophorbide-a and bacteriopurpurinimide by circular dichroism spectroscopy and its correlation with in vivo photosensitizing efficacy
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An approach to heterobifunctional poly(ethyleneglycol) bioconjugates
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An oxidatively releasable caging group that senses lipid peroxidation
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New series of potent δ-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif
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Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases
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A thiolate ligand on a cytochrome P-450 mimic permits the use of simple environmentally benign oxidants for biomimetic steroid hydroxylation in water
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Two-step enzymatic synthesis of UDP-N-acetylgalactosamine
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New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors
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Efficient synthesis of C-terminal modified peptide ketones for chemical ligations
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Pharmacophoric features and Ca2+ ion holding capacity of verapamil
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Conformationally restricted analogs of Combretastatin A-4 derived from SU5416
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Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors
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SAR studies of 2-arylthiazolidine-4-carboxylic acid amides: A novel class of cytotoxic agents for prostate cancer
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O-Methylglucogalloyl esters: Synthesis and evaluation of their antimycotic activity
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Novel peptide derivatives of bleomycin A5: Synthesis, antitumor activity and interaction with DNA
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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
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Instructions to contributors
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Design and synthesis of new bis-pyridinium oxime reactivators for acetylcholinesterase inhibited by organophosphorous nerve agents
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Synthesis and structure–activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists
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New inhibitors of rabbit muscle triose-phosphate isomerase
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Biological evaluation of Tyr6 and Ser7 modified drosocin analogues
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Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism
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Synthesis, in vivo and in vitro biological activity of novel azaline B analogs
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Azinomycin inspired bisepoxides: influence of linker structure on in vitro cytotoxicity and DNA interstrand cross-linking
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Anti-malarial activity of Baylis–Hillman adducts from substituted 2-chloronicotinaldehydes
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Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13
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A micromethod for the stereochemical analysis of fatty acid desaturase-mediated sulfoxidation reactions
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Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines
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The evaluation of 2,8-disubstituted benzoxazinone derivatives as anti-inflammatory and anti-platelet aggregation agents
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Synthesis and evaluation of 6-hydroxy-7-methoxy-4-chromanone- and chroman-2-carboxamides as antioxidants
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Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase
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Use of PROTACS as molecular probes of angiogenesis
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Chiral discrimination in binding of enantiomers of 2-(aminoalkoxy)-substituted 4-(2-thienyl)pyrimidines and 4,6-bis(2-thienyl)pyrimidines with duplex DNA
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Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives
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Redox-responsive and calcium-dependent switching of glycosyldisulfide interactions with Concanavalin A
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Instructions to contributors
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