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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Tin(IV) complexes of pyrrolidinedithiocarbamate: synthesis, characterisation and antifungal activity
Fulltext Access 6 Pages 2005
Synthesis and antibacterial activity of some new 1-heteroaryl-5-amino-4-phenyl-3-trifluoromethylpyrazoles
Fulltext Access 6 Pages 2005
Synthesis and in vivo analgesic and anti-inflammatory activity of some bi heterocyclic coumarin derivatives
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Fluorescein-labeled sinistrin as marker of glomerular filtration rate
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Synthesis, characterization and antimicrobial activity of some substituted 1,2,3-triazoles
Fulltext Access 6 Pages 2005
Facile synthesis of active antitubercular, cytotoxic and antibacterial agents: a Michael addition approach
Fulltext Access 6 Pages 2005
Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates
Fulltext Access 6 Pages 2005
Enhancement of drug affinity for cell membranes by conjugation with lipoamino acids. I. Synthesis and biological evaluation of lipophilic conjugates of tranylcypromine
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Copper(II) complexes with substituted thiosemicarbazones of thiophene-2-carboxaldehyde: synthesis, characterization and antiamoebic activity against E. histolytica
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Solubility of nicotinic acid in polyamidoamine dendrimer solutions
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Synthesis and antinociceptive activity of some substituted-{5-[2-(1,2,3,4-tetrahydrocarbazol-9-yl)ethyl]tetrazol-1-yl}alkanones
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Synthesis and antimalarial activities of some furoxan sulfones and related furazans
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Synthesis of new series of 1-Aryl-1,4-dihydro-4-oxo-6-methyl pyridazine-3-carboxylic acid as potential antibacterial agents
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Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives
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Sequence specific recognition of DNA by tailor-made hairpin conjugates of achiral seco-cyclopropaneindoline-2-benzofurancarboxamide and pyrrole–imidazole polyamides
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Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones
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Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff’s bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes
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Structure-based design and synthesis of pyrazinones containing novel P1 ‘side pocket’ moieties as inhibitors of TF/VIIa
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Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator
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In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation: Carbon analogs of (−)-cytisine
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Discovery and structure–activity relationships of novel sulfonamides as potent PTP1B inhibitors
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Synthesis and antipicornavirus activity of (R)- and (S)-1-[5-(4′-chlorobiphenyl-4-yloxy)-3-methylpentyl]-3-pyridin-4-yl-imidazolidin-2-one
Fulltext Access 6 Pages 2005
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists
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Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists
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New dual inhibitors of EGFR and HER2 protein tyrosine kinases
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Anti-tumor-promoting activity of simple models of galactoglycerolipids with branched and unsaturated acyl chains
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Novel heterocyclic thyromimetics
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2,3-Diarylthiophenes as selective EP1 receptor antagonists
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Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides
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Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13)
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Conformational analysis of rhazinilam and three-dimensional quantitative structure-activity relationships of rhazinilam analogues
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Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA)
Fulltext Access 6 Pages 2005
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists
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Molecular docking of the highly hypolipidemic agent α-asarone with the catalytic portion of HMG-CoA reductase
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Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane
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Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides
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Novel use of chemical shift in NMR as molecular descriptor: a first report on modeling carbonic anhydrase inhibitory activity and related parameters
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Inclusion complexes of N-sulfamoyloxazolidinones with β-cyclodextrin
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Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
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Generation of predictive pharmacophore model for SARS-coronavirus main proteinase
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Syntheses and antibacterial activity of a series of 3-(pyridine-3-yl)-2-oxazolidinone
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Synthesis and antimycobacterial activity of 2-substituted halogenobenzimidazoles
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Synthesis and biological evaluation of 6/7-exo-methyl-3β-(4-iodo)phenyltropane-2β-carboxylic acid methyl esters
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Synthetic studies on cyclic octapeptides: Yunnanin F and Hymenistatin
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Synthesis, pharmacological activity and hydrolytic behavior of glyceride prodrugs of ibuprofen
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Structural studies and cytotoxic activity of N(4)-phenyl-2-benzoylpyridine thiosemicarbazone Sn(IV) complexes
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Novel bidentate complexes of Cu(II) derived from 5-nitrofuran-2-carboxaldehyde thiosemicarbazones with antiamoebic activity against E. histolytica
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A solid-phase approach to DDB derivatives
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Synthesis and cytotoxic evaluation of certain 4-anilino-2-phenylquinoline derivatives
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Chemotherapy of leishmaniasis part II: synthesis and bioevaluation of substituted arylketene dithioacetals as antileishmanial agents
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Determination of human serum albumin using an intramolecular charge transfer fluorescence probe: 4′-Dimethylamino-2,5-dihydroxychalcone
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Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase
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Indole- and indoline-based kainate analogues with antagonist activity at ionotropic glutamate receptors
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A linear discrimination analysis based virtual screening of trichomonacidal lead-like compounds: Outcomes of in silico studies supported by experimental results
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Carbonic anhydrase inhibitors: Inhibition of the transmembrane isozyme XIV with sulfonamides
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New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities
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Structure–activity relationship study of novel necroptosis inhibitors
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Structure-based design of 7-carbamate analogs of geldanamycin
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Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1
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Privileged structure based ligands for melanocortin receptors—Substituted benzylic piperazine derivatives
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Topological model for the prediction of MRP1 inhibitory activity of pyrrolopyrimidines and templates derived from pyrrolopyrimidine
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Synthesis and SAR of highly selective MMP-13 inhibitors
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Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives
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Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
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Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5
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Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors
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Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: Discovery of the dihydropyridazinone motif
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A prodrug system for hydroxylamines based on esterase catalysis
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Reduced cardiac side-effect potential by introduction of polar groups: Discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo
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Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity
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Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides
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Homology modeling and docking study of cyclin-dependent kinase (CDK) 10
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Quantitative structure-activity relationship studies for antioxidant hydroxybenzalacetones by quantum chemical- and 3-D-QSAR(CoMFA) analyses
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Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid
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Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity
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Structure–activity relationships of bivalent aminoglycosides and evaluation of their microbiological activities
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Exploring the connection unit in the HDAC inhibitor pharmacophore model: Novel uracil-based hydroxamates
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Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids
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Radical scavenging activity of protein from tentacles of jellyfish Rhopilema esculentum
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Design, synthesis and structure–activity relationships of 6-O-arylpropargyl diazalides with potent activity against multidrug-resistant Streptococcus pneumoniae
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Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice
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Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid
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Pyrrolo[1,2-a][1,4]benzodiazepine: A novel class of non-azole anti-dermatophyte anti-fungal agents
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Potential new antitumor agents from an innovative combination of camphorato, a ramification of traditional Chinese medicine, with a platinum moiety
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Rhodanine derivatives as inhibitors of JSP-1
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The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors
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Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties
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Biaryl isoxazolinone antibacterial agents
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QSAR analyses of conformationally restricted 1,5-diaryl pyrazoles as selective COX-2 inhibitors: application of connection table representation of ligands
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Benzothiazolium compounds: novel classes of inhibitors that suppress the nitric oxide production in RAW264.7 cells stimulated by LPS/IFNγ
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Bicyclic nucleoside inhibitors of Varicella–Zoster virus: The effect of branching in the p-alkylphenyl side chain
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A physicogenetic method to assign ligand-binding relationships between 7TM receptors
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1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists
Fulltext Access 6 Pages 2005
Structure–activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists
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A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists
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Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating thioureido-sulfanilyl scaffolds
Fulltext Access 6 Pages 2005
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides—a new zinc-binding function in the design of inhibitors
Fulltext Access 6 Pages 2005
Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-thiadiazole- and 1,2,4-triazole-thiols
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Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies
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