Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles Fulltext Access 5 Pages 2005
Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes Fulltext Access 5 Pages 2005
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors Fulltext Access 5 Pages 2005
Antiviral 6-amino-quinolones: Molecular basis for potency and selectivity Fulltext Access 5 Pages 2005
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists Fulltext Access 5 Pages 2005
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors Fulltext Access 5 Pages 2005
Novel, selective indole-based ECE inhibitors: Lead optimization via solid-phase and classical synthesis Fulltext Access 5 Pages 2005
Correlation of cytotoxic activity of betulinines and their hydroxy analogues Fulltext Access 5 Pages 2005
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P2′ moiety with improved potency Fulltext Access 5 Pages 2005
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors: Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with benzo[b]thiophene 1,1-dioxide sulfonamides Fulltext Access 5 Pages 2005
3-(2-Aminoethyl)pyridine analogs as α4β2 nicotinic cholinergic receptor ligands Fulltext Access 5 Pages 2005
Carbonic anhydrase inhibitors: Inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides Fulltext Access 5 Pages 2005
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1 Fulltext Access 5 Pages 2005
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2 Fulltext Access 5 Pages 2005
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents Fulltext Access 5 Pages 2005
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists Fulltext Access 5 Pages 2005
Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists Fulltext Access 5 Pages 2005
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity Fulltext Access 5 Pages 2005
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex Fulltext Access 5 Pages 2005
Total and semisynthesis and in vitro studies of both enantiomers of 20-fluorocamptothecin Fulltext Access 5 Pages 2005
Parallel synthesis and biological evaluation of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells Fulltext Access 5 Pages 2005
Novel C2–C3′ N-peptide linked macrocyclic taxoids. Part 1: Synthesis and biological activities of docetaxel analogues with a peptide side chain at C3′ Fulltext Access 5 Pages 2005
A strategy to profile prime and non-prime proteolytic substrate specificity Fulltext Access 5 Pages 2005
Inhibition of hydrogen peroxide-induced necrotic cell death with 3-amino-2-indolylmaleimide derivatives Fulltext Access 5 Pages 2005
Structure–activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors Fulltext Access 5 Pages 2005
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: Orally active prostacyclin mimetics. Part 3 Fulltext Access 5 Pages 2005
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease Fulltext Access 5 Pages 2005
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential Fulltext Access 5 Pages 2005
Quaternary salts of 4,3′ and 4,4′ bis-pyridinium monooximes: Synthesis and biological activity Fulltext Access 5 Pages 2005
Total asymmetric synthesis of (−)-conduramine B-1 and of its enantiomer. N-Benzyl derivatives of conduramine B-1 are β-glucosidase inhibitors Fulltext Access 5 Pages 2005
Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors Fulltext Access 5 Pages 2005
4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17β-hydroxysteroid dehydrogenase. Part 2. SAR Fulltext Access 5 Pages 2005
Discovery of potent and selective orally bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors Fulltext Access 5 Pages 2005
An efficient synthesis of argifin: A natural product chitinase inhibitor with chemotherapeutic potential Fulltext Access 5 Pages 2005
Synthesis of a small library of diketopiperazines as potential inhibitors of calpain Fulltext Access 5 Pages 2005
Stereospecific synthesis and mass spectrometry of 5,6-trans-epoxy-8Z,11Z,14Z-eicosatrienoic acid Fulltext Access 5 Pages 2005
Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: Synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites Fulltext Access 5 Pages 2005
Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase Fulltext Access 5 Pages 2005
Synthesis and antiamoebic activity of new oxime ether derivatives containing 2-acetylpyridine/2-acetylfuran Fulltext Access 5 Pages 2005
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: Potent, selective, orally bioavailable 5-HT1 receptor ligands Fulltext Access 5 Pages 2005
Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor Fulltext Access 5 Pages 2005
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates Fulltext Access 5 Pages 2005
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities Fulltext Access 5 Pages 2005
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: Inhibition of interleukin-1β-converting enzyme Fulltext Access 5 Pages 2005
Structural elucidation of A-74528, an inhibitor for 2â²,5â²-phosphodiesterase isolated from Streptomyces sp. Fulltext Access 5 Pages 2005
Synthesis of cationic β-vinyl substituted meso-tetraphenylporphyrins and their in vitro activity against herpes simplex virus type 1 Fulltext Access 5 Pages 2005
Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor Fulltext Access 5 Pages 2005
(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors Fulltext Access 5 Pages 2005
(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors Fulltext Access 5 Pages 2005
Deoxyribosyl analogues of methionyl and isoleucyl sulfamate adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of quinoxaline-5,8-diones that inhibit vascular smooth muscle cell proliferation Fulltext Access 5 Pages 2005
Syntheses of NAMDA derivatives inhibiting NO production in BV-2 cells stimulated with lipopolysaccharide Fulltext Access 5 Pages 2005
6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-γ activators Fulltext Access 5 Pages 2005
(2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents Fulltext Access 5 Pages 2005
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy Fulltext Access 5 Pages 2005
Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport Fulltext Access 5 Pages 2005
Design, synthesis and ribosome binding of chloramphenicol nucleotide and intercalator conjugates Fulltext Access 5 Pages 2005
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands Fulltext Access 5 Pages 2005
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder Fulltext Access 5 Pages 2005
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of alkyl derivatives of the glycopeptide antibiotic A40926 and their amides Fulltext Access 5 Pages 2005
Synthesis of novel curcumin mimics with asymmetrical units and their anti-angiogenic activity Fulltext Access 5 Pages 2005
Site-specific immobilization of proteins in a microarray using intein-mediated protein splicing Fulltext Access 5 Pages 2005
Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-β Fulltext Access 5 Pages 2005
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold Fulltext Access 5 Pages 2005
Geometry, topology, and atom-weights assembly descriptors to predicting A1 adenosine receptors agonists Fulltext Access 5 Pages 2005
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues Fulltext Access 5 Pages 2005
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer Fulltext Access 5 Pages 2005
Macrolactonization catalyzed by the terminal thioesterase domain of the nonribosomal peptide synthetase responsible for lichenysin biosynthesis Fulltext Access 5 Pages 2005
Structure–activity relationships of arylbenzofuran H3 receptor antagonists Fulltext Access 5 Pages 2005
1-((S)-γ-Substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors Fulltext Access 5 Pages 2005
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers Fulltext Access 5 Pages 2005
In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: Part 14 Fulltext Access 5 Pages 2005
4-Alkyl and 4,4′-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives as new inhibitors of bacterial cell wall biosynthesis Fulltext Access 5 Pages 2005
Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine Fulltext Access 5 Pages 2005
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1 Fulltext Access 5 Pages 2005
Metalloform-selective inhibition: Synthesis and structure–activity analysis of Mn(II)-form-selective inhibitors of Escherichia coli methionine aminopeptidase Fulltext Access 6 Pages 2005
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents Fulltext Access 6 Pages 2005
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors Fulltext Access 6 Pages 2005
Synthesis of selective SRPK-1 inhibitors: Novel tricyclic quinoxaline derivatives Fulltext Access 6 Pages 2005
Recognition of a 10 base pair sequence of DNA and stereochemical control of the binding affinity of chiral hairpin polyamide–Hoechst 33258 conjugates Fulltext Access 6 Pages 2005
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes Fulltext Access 6 Pages 2005
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors Fulltext Access 6 Pages 2005