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Daneshyari Drug Discovery Journas Latest Articles

Drug Discovery Research Articles

Pelseneeriol-1 and -2: new furanosesquiterpene alcohols from porostome nudibranch Doriopsilla pelseneeri
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Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase
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Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties
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Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (β-secretase)
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Combinatorial approaches towards the discovery of new tryptase inhibitors
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Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines
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Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II
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An efficient synthesis of 7-hydroxy-2,6-dimethylchromeno[3,4-d]oxazol-4-one-a protected fragment of novenamine
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Graphical contents list
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Nucleophilic addition to dimethylvinylphosphine sulfide as a convenient route to polydentate ligands containing the 2-dimethylphosphinoethyl unit
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Stereoselective total synthesis of (S)-Virol C and (S)-1-dehydroxyvirol A
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Anthracene derivatives bearing two urea groups as fluorescent receptors for anions
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Graphical contents list
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Synthesis and in vitro study of novel Mannich bases as antibacterial agents
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Chemo-, regio- and stereoselective Diels-Alder reactions of EWG bearing thiophene-1,1-dioxides
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Silicaphosphine (Silphos): a filterable reagent for the conversion of alcohols and thiols to alkyl bromides and iodides
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Applications of surfactant-modified clays to synthetic organic chemistry
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Preparation of new heterotopic ligands
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Exploiting the Maitland-Japp reaction: a synthesis of (±)-centrolobine
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The microbiological transformation of steroidal saponins by Curvularia lunata
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Photoreduction of imines. An environmentally friendly approach to obtain amines
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Graphical contents list
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Amine side arm effect on the ion selectivity of 12-crown-O3N derivatives with an amine arm in aqueous and acetonitrile solutions
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Apteniols A-F, oxyneolignans from the leaves of Aptenia cordifolia
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Aza Diels-Alder reactions utilizing 4-iodo-2-trimethylsilyloxy-butadiene
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Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates
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Synthesis of a library of benzoindolizines using poly(ethylene glycol) as soluble support
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A novel series of potent γ-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core
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Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX
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Benzoyl 2-methyl indoles as selective PPARγ modulators
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Synthesis and antimalarial evaluation of new N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives
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Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists
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Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors
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1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR
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Tellurium-based cysteine protease inhibitors: evaluation of novel organotellurium(IV) compounds as inhibitors of human cathepsin B
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A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists
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Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent
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Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates
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Graphical contents list
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New conformationally locked bicyclic N,O-nucleoside analogues of antiviral drugs
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Identification of putative metabolites of docosahexaenoic acid as potent PPARγ agonists and antidiabetic agents
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3,4-Disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity
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Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction
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Design and synthesis of novel 9-substituted-7-aryl-3,4,5,6-tetrahydro-2H-pyrido[4,3-b]- and [2,3-b]-1,5-oxazocin-6-ones as NK1 antagonists
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Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists
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Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase
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Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity
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Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives
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N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP
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Design of dantrolene-derived probes for radioisotope-free photoaffinity labeling of proteins involved in the physiological Ca2+ release from sarcoplasmic reticulum of skeletal muscle
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Ring opening of 2-(bromomethyl)-1-sulfonylaziridines towards 1,3-heteroatom substituted 2-aminopropane derivatives
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Hetero Diels-Alder reactions (HDAR) of α,α′-dioxothiones on solid support
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Mannich-type reaction of (1-methoxy-2-methylpropenyloxy)trimethylsilane with arylaldehydes and aromatic amines catalyzed by perfluorinated rare earth metal salts in fluorous phase
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Synthesis of naturally occurring bioactive butyrolactones: maculalactones A-C and nostoclide I
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Total synthesis of cimiracemate B and analogs
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Ring-closure reactions through intramolecular substitution of thiophenoxide by oxygen and nitrogen nucleophiles: simple stereospecific synthesis of 4,5-dihydroisoxazoles and 4,5-dihydropyrazoles
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Simple and efficient preparation of sterically protected 1,4-diphosphafulvenes
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Graphical contents list
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Nitrosation of hydrochlorothiazide and the modes of binding of the N-nitroso derivative with two macrocycles possessing an 18-membered crown ether cavity
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Halogen-lithium exchange between substituted dihalobenzenes and butyllithium: application to the regioselective synthesis of functionalized bromobenzaldehydes
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Stereoselective synthesis of (2R,3S,4S)-3-hydroxy-4-methyl-2-tetradecyl-4-butanolide starting from 2,5-anhydro-d-mannitol
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Selective palladium-catalyzed amination of β-chloroacroleins by substituted anilines
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Graphical contents list
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A novel 3,4-dihydroisoquinoline annulation: expedient access to isoquinoline heterocycles
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Synthesis and interfacial properties of amphiphilic β-cyclodextrins and their substitution at the O-6 position with a mono bio-recognisable galactosyl antenna
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Facile synthesis of α,β-acetylenic ketones and 2,5-disubstituted furans: consecutive activation of triple and double bond with ZnBr2 toward the synthesis of furan ring
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Stereoselective synthesis of a 12-acetoxyazadiradione analogue
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Reductive metalation of 1,2-diaryl-substituted ethenes: synthetic applications
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An approach to the synthesis of chemically modified bisazocalix[4]arenes and their extraction properties
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Synthesis of furo[2,3-c]-2,7-naphthyridine derivatives via domino heterocyclization reaction
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A mild and efficient aza-Diels-Alder reaction of N-benzhydryl imines with trans-1-methoxy-2-methyl-3-trimethylsiloxybuta-1,3-diene catalyzed by Yb(OTf)3
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Comparison of 'classic' 99mTc-DTPA, 99mTc(CO)3-DTPA and 99mTc(CO)2(NO)-DTPA
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Diterpenoids from Coprinus heptemerus
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Highly efficient one-pot synthesis of 1-substituted-1,2,3,4-tetrahydropyrazino[1,2-a]indoles
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Palladium catalyzed Suzuki cross-coupling reactions using N,O-bidentate ligands
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DTBB-catalysed lithiation of 1,2-bis(phenylsulfanyl)ethene: does 1-lithio-2-phenylsulfanylethene really exist?
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Direct synthesis of new arylanthranilic acids via a Suzuki cross-coupling reaction from iodoisatins
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Preparation of polystyrene-supported soluble palladacycle catalyst for Heck and Suzuki reactions
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A chemoenzymic approach to the epoxidation of alkenes in aqueous media
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Proton affinities and relative basicities of two 1,4,7-triazacyclononanes, Me3TACN and TP-TACN. Quantum-chemical ab initio calculations, solution measurements, and the structure of [TP-TACN·2H]2+ in the solid state
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Tetrazolecalix[4]arenes as new ligands for palladium(II)
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The effect of coordination on the reaction of N-tosyl imines with diethylzinc
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Diastereoselectivity-switchable and regiospecific hetero Diels-Alder reaction of N-sulfinylper(poly)fluoroalkanesulfinamides with dienes
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Understanding the enantioselectivity of a heterogeneous catalyst: the influence of ligand loading and of silica passivation
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A convenient and efficient synthesis of (S)-lysine and (S)-arginine homologues via olefin cross-metathesis
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A borderline case between meso and stable C1: an axially chiral, yet configurationally semi-stable biphenyl with two oppositely configured [10]paracyclophane portions
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Biocatalytic and chemical investigations in the synthesis of sucrose analogues
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Solid-phase synthesis of 6-hydroxy-2,4-diaminoquinazolines
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Synthesis and characterisation of N-1,10-phenanthrolin-5-ylalkylamides and their photosensitising heteroleptic Ru(II) complexes
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Deallyloxy- and debenzyloxycarbonylation of protected alcohols, amines and thiols via a naphthalene-catalysed lithiation reaction
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Synthesis of thiazino[6,5-b]indole derivatives, analogues of the phytoalexin cyclobrassinin. A new method for preparation of 3-aminomethylindole
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New potent cytotoxic lamellarin alkaloids from Indian ascidian Didemnum obscurum
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Synthesis of 4-halophosphaisocoumarins via halocyclization of 2-(1-alkynyl)phenylphosphonates
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Biomimic transformation of resveratrol
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Graphical contents list
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Versatile acenaphtho[1,2-b]pyrrol-carbonitriles as a new family of heterocycles: diverse SNArH reactions, cytotoxicity and spectral behavior
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Reduction of alkyl and vinyl sulfonates using the CuCl2·2H2O-Li-DTBB(cat.) system
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Bis- and tetracalix[4]arenes in the partial cone conformation: synthesis, structure and RCM reactions
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Shielding effect of thioether C-S bond from proton chemical shifts of 4-thia-5α- and 4-thia-5β-androstane-17-ones
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Unusual asymmetric oxidation of sulfide; the diastereoselective oxidation of prochiral sulfide-chiral acid salt with hydrogen peroxide without metal
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