104 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.
University of Pennsylvania
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
University of Pennsylvania
Synthesis and evaluation of N8-acetylspermidine analogues as inhibitors of bacterial acetylpolyamine amidohydrolase.
University of Pennsylvania
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [(125)I]Flip-IDAM, (2-((2-((dimethylamino)methyl)-4-iodophenyl)thio)phenyl)methanol.
University of Pennsylvania
Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17ß-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.
University of Pennsylvania
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.
University of Pennsylvania
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.
University of Pennsylvania
Hydrophobic effect and hydrogen bonds account for the improved activity of a complement inhibitor, compstatin.
University of Pennsylvania
F-18 stilbenes as PET imaging agents for detecting beta-amyloid plaques in the brain.
University of Pennsylvania
Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
University of Pennsylvania
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
University of Pennsylvania
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
University of Pennsylvania
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.
University of Pennsylvania
Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants.
University of Pennsylvania
Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands.
University of Pennsylvania
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand.
University of Pennsylvania
R2 C-terminal peptide inhibition of mammalian and yeast ribonucleotide reductase.
University of Pennsylvania
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.
University of Pennsylvania
Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand.
University of Pennsylvania
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
University of Pennsylvania
Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.
University of Pennsylvania
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
University of Pennsylvania
Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.
University of Pennsylvania
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.
University of Pennsylvania
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.
University of Pennsylvania
Synthesis of new (-)-bestatin-based inhibitor libraries reveals a novel binding mode in the S1 pocket of the essential malaria M1 metalloaminopeptidase.
University of Pennsylvania
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17ß-hydroxysteroid dehydrogenase (AKR1C3).
University of Pennsylvania
2-aminoimidazole amino acids as inhibitors of the binuclear manganese metalloenzyme human arginase I.
University of Pennsylvania
Iodophenyl tagged sphingosine derivatives: synthesis and preliminary biological evaluation.
University of Pennsylvania
2-(2'-((dimethylamino)methyl)-4'-(fluoroalkoxy)-phenylthio)benzenamine derivatives as serotonin transporter imaging agents.
University of Pennsylvania
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.
University of Pennsylvania
Creation of a Peptide Antagonist of the GFRAL-RET Receptor Complex for the Treatment of GDF15-Induced Malaise.
University of Pennsylvania
Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres.
University of Pennsylvania
Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
University of Pennsylvania
Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
University of Pennsylvania
Design, synthesis, and evaluation of octahydropyranopyrrole-based inhibitors of mammalian ribonucleotide reductase.
University of Pennsylvania
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.
University of Pennsylvania
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.
University of Pennsylvania
Identification of gp120 Residue His105 as a Novel Target for HIV-1 Neutralization by Small-Molecule CD4-Mimics.
University of Pennsylvania
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.
University of Pennsylvania
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.
University of Pennsylvania
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).
University of Pennsylvania
Isomerization of (Z,Z) to (E,E)1-bromo-2,5-bis-(3-hydroxycarbonyl-4-hydroxy)styrylbenzene in strong base: probes for amyloid plaques in the brain.
University of Pennsylvania
Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates.
University of Pennsylvania
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
University of Pennsylvania
Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.
University of Pennsylvania
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.
University of Pennsylvania
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.
University of Pennsylvania
Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.
University of Pennsylvania
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.
University of Pennsylvania
Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents.
University of Pennsylvania
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.
University of Pennsylvania
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
University of Pennsylvania
Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.
University of Pennsylvania
Synthesis and characterization of technetium-99m-labeled tropanes as dopamine transporter-imaging agents.
University of Pennsylvania
Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases.
University of Pennsylvania
Synthesis and optical resolution of (R)- and (S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand.
University of Pennsylvania
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.
University of Pennsylvania
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.
University of Pennsylvania
The β-Amyloid Hypothesis in Alzheimer's Disease: Seeing Is Believing.
University of Pennsylvania
Multidentate (18)F-polypegylated styrylpyridines as imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA).
University of Pennsylvania
Identification of triazinoindol-benzimidazolones as nanomolar inhibitors of the Mycobacterium tuberculosis enzyme TDP-6-deoxy-d-xylo-4-hexopyranosid-4-ulose 3,5-epimerase (RmlC).
University of Pennsylvania
18F stilbenes and styrylpyridines for PET imaging of A beta plaques in Alzheimer's disease: a miniperspective.
University of Pennsylvania
Synthesis and evaluation of indolinyl- and indolylphenylacetylenes as PET imaging agents for beta-amyloid plaques.
University of Pennsylvania
Radioiodinated aza-diphenylacetylenes as potential SPECT imaging agents for beta-amyloid plaque detection.
University of Pennsylvania
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.
University of Pennsylvania
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques.
University of Pennsylvania
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.
University of Pennsylvania
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.
University of Pennsylvania
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.
University of Pennsylvania
Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine.
University of Pennsylvania
Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.
University of Pennsylvania
Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.
University of Pennsylvania
(+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent.
University of Pennsylvania
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.
University of Pennsylvania
Indazolecarboxamides, processes for their preparation, pharmaceutical preparations comprising them and their use for producing medicaments
Bayer Pharma Aktiengesellschaft
Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
Shanghai Yingli Pharmaceutical
Imide and acylurea derivatives as modulators of the glucocorticoid receptor
Bristol-Myers Squibb
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Boehringer Ingelheim Pharmaceuticals
Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors.
Universita Di Pisa
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Kudos Pharmaceuticals
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.
University of California Berkeley
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis
Wyeth Research