Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives Fulltext Access 5 Pages 2005
4-Fluorosulfonylpiperidines: Selective 5-HT2A ligands for the treatment of insomnia Fulltext Access 5 Pages 2005
Synthesis and bioactivities of two multiple antigen peptides as potential vaccine against schistosoma Fulltext Access 5 Pages 2005
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production Fulltext Access 5 Pages 2005
3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2) Fulltext Access 5 Pages 2005
Synthesis and anthelmintic activity of 7-substituted 3,4a-dimethyl-4a,5a,8a,8b-tetrahydro-6H-pyrrolo[3â²,4â²:4,5]furo[3,2-b]pyridine-6,8(7H)-diones Fulltext Access 5 Pages 2005
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED Fulltext Access 5 Pages 2005
Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives Fulltext Access 5 Pages 2005
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase Fulltext Access 5 Pages 2005
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor Fulltext Access 5 Pages 2005
The development of monocyclic pyrazolone based cytokine synthesis inhibitors Fulltext Access 5 Pages 2005
Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure–activity relationships Fulltext Access 5 Pages 2005
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A2A antagonists. Part 1 Fulltext Access 5 Pages 2005
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor Fulltext Access 5 Pages 2005
Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain Fulltext Access 5 Pages 2005
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action Fulltext Access 5 Pages 2005
A structural screening approach to ketoamide-based inhibitors of cathepsin K Fulltext Access 5 Pages 2005
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors Fulltext Access 5 Pages 2005
Effects of linking 15-zinc finger domains on DNA binding specificity and multiple DNA binding modes Fulltext Access 5 Pages 2005
Structure–activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption Fulltext Access 5 Pages 2005
Induction of apoptosis by a novel indirubin-5-nitro-3′-monoxime, a CDK inhibitor, in human lung cancer cells Fulltext Access 5 Pages 2005
Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series Fulltext Access 5 Pages 2005
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain Fulltext Access 5 Pages 2005
Ketoheterocycle-based inhibitors of cathepsin K: A novel entry into the synthesis of peptidic ketoheterocycles Fulltext Access 5 Pages 2005
Design, synthesis and ribosome binding of chloramphenicol nucleotide and intercalator conjugates Fulltext Access 5 Pages 2005
Evaluation of a pulmonary graphical display in the medical intensive care unit: An observational study Fulltext Access 5 Pages 2005
Prediction of vascular tissue engineering results with artificial neural networks 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 of cationic β-vinyl substituted meso-tetraphenylporphyrins and their in vitro activity against herpes simplex virus type 1 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
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors 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
Chemical modification of the naphthoyl 3-position of JWH-015: In search of a fluorescent probe to the cannabinoid CB2 receptor Fulltext Access 5 Pages 2005
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands Fulltext Access 5 Pages 2005
Antibiotics GE23077, novel inhibitors of bacterial RNA polymerase. Part 3: Chemical derivatization Fulltext Access 5 Pages 2005
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives Fulltext Access 5 Pages 2005
Functionalized head-to-head hairpin polyamides: Synthesis, double-stranded DNA-binding activity and affinity Fulltext Access 5 Pages 2005
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis Fulltext Access 5 Pages 2005
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists Fulltext Access 5 Pages 2005
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: Discovery of potent S1P1 receptor agonists Fulltext Access 5 Pages 2005
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors Fulltext Access 5 Pages 2005
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase Fulltext Access 5 Pages 2005
Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1 Fulltext Access 5 Pages 2005
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt Fulltext Access 5 Pages 2005
Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles Fulltext Access 5 Pages 2005
Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist Fulltext Access 5 Pages 2005
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists Fulltext Access 5 Pages 2005
Design, synthesis, and structure–activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis Fulltext Access 5 Pages 2005
Hydantoin derivative formation from oxidation of 7,8-dihydro-8-oxo-2′-deoxyguanosine (8-oxodG) and incorporation of 14C-labeled 8-oxodG into the DNA of human breast cancer cells Fulltext Access 5 Pages 2005
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells Fulltext Access 5 Pages 2005
Screening of active compounds as neuromedin U2 receptor agonist from natural products Fulltext Access 5 Pages 2005
An efficient synthesis of aryloxyphenyl cyclopropyl methanones: a new class of anti-mycobacterial agents Fulltext Access 5 Pages 2005
Hepatitis C virus NS3-4A serine protease inhibitors: Use of a P2–P1 cyclopropyl alanine combination for improved potency Fulltext Access 5 Pages 2005
Facile synthesis and PET imaging of a novel potential heart acetylcholinesterase tracer N-[11C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2â²,2â²-diphenylpropionoxymethyl)pyridinium Fulltext Access 5 Pages 2005
Synthesis and antibacterial activity of N-(5-benzylthio-1,3,4-thiadiazol-2-yl) and N-(5-benzylsulfonyl-1,3,4-thiadiazol-2-yl)piperazinyl quinolone derivatives Fulltext Access 5 Pages 2005
Synthesis and cytotoxic activity of platinum complex immobilized by branched polyethylene glycol Fulltext Access 5 Pages 2005
Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors Fulltext Access 5 Pages 2005
Synthesis and evaluation of anti-HIV activity of isatin β-thiosemicarbazone derivatives Fulltext Access 5 Pages 2005
Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors Fulltext Access 5 Pages 2005
Pentacyclic triterpenes. Part 1: The first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases Fulltext Access 5 Pages 2005
Radiosynthesis of carbon-11-labeled camptothecin derivatives as potential positron emission tomography tracers for imaging of topoisomerase I in cancers Fulltext Access 5 Pages 2005
Synthesis of an N-acyl sulfamate analog of luciferyl-AMP: A stable and potent inhibitor of firefly luciferase Fulltext Access 5 Pages 2005
SAR and biological evaluation of novel trans-3,4-dimethyl-4-arylpiperidine derivatives as opioid antagonists Fulltext Access 5 Pages 2005
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series Fulltext Access 5 Pages 2005
Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3 Fulltext Access 5 Pages 2005
Synthesis of doxorubicin–peptide conjugate with multidrug resistant tumor cell killing activity Fulltext Access 5 Pages 2005
Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2″-hydroxy naphthalen-1″-yl)-1,5-diphenyl-2-pyrazolines Fulltext Access 5 Pages 2005
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor Fulltext Access 5 Pages 2005
High affinity iron(III) scavenging by a novel hexadentate 3-hydroxypyridin-4-one-based dendrimer: Synthesis and characterization Fulltext Access 5 Pages 2005
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists Fulltext Access 5 Pages 2005
Synthesis and biological evaluation of novel (l)-α-amino acid methyl ester, heteroalkyl, and aryl substituted 1,4-naphthoquinone derivatives as antifungal and antibacterial agents Fulltext Access 5 Pages 2005
Bis(indole) alkaloids as sortase A inhibitors from the sponge Spongosorites sp. Fulltext Access 5 Pages 2005
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides Fulltext Access 5 Pages 2005
Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes Fulltext Access 5 Pages 2005
Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): Efficacy in an animal model for schizophrenia Fulltext Access 5 Pages 2005
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles Fulltext Access 5 Pages 2005
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry Fulltext Access 5 Pages 2005
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities Fulltext Access 5 Pages 2005
Structure–activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads Fulltext Access 5 Pages 2005