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The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.

Virginia Commonwealth University

Synthesis and pharmacological evaluation of ether and related analogues of delta 8-, delta 9-, and delta 9,11-tetrahydrocannabinol.

Virginia Commonwealth University

A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.

Virginia Commonwealth University

Design, synthesis, and biological evaluation of substrate-competitive inhibitors of C-terminal Binding Protein (CtBP).

Virginia Commonwealth University

Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.

Virginia Commonwealth University

Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine.

Virginia Commonwealth University

Exploration on natural product anibamine side chain modification toward development of novel CCR5 antagonists and potential anti-prostate cancer agents.

Virginia Commonwealth University

Synthesis and Characterization of 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC) and Its Analogues as Non-nitrogenous 5-HT2B Ligands.

Virginia Commonwealth University

Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.

Virginia Commonwealth University

A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.

Virginia Commonwealth University

Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.

Virginia Commonwealth University

Design, syntheses, and characterization of piperazine based chemokine receptor CCR5 antagonists as anti prostate cancer agents.

Virginia Commonwealth University

Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors.

Virginia Commonwealth University

Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.

Virginia Commonwealth University

5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): a novel non-nitrogenous ligand for 5-HT2B receptor.

Virginia Commonwealth University

Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.

Virginia Commonwealth University

Design, syntheses, and characterization of pharmacophore based chemokine receptor CCR5 antagonists as anti prostate cancer agents.

Virginia Commonwealth University

2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.

Virginia Commonwealth University

Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.

Virginia Commonwealth University

Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.

Virginia Commonwealth University

On scaffold hopping: challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans.

Virginia Commonwealth University

Deconstruction of thea4ß2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine.

Virginia Commonwealth University

alpha4beta2 nACh receptor pharmacophore models.

Virginia Commonwealth University

3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.

Virginia Commonwealth University

Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selectiveµ opioid receptor Agents.

Virginia Commonwealth University

Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.

Virginia Commonwealth University

Structure activity relationship studies of natural product chemokine receptor CCR5 antagonist anibamine toward the development of novel anti prostate cancer agents.

Virginia Commonwealth University

The potential role of anibamine, a natural product CCR5 antagonist, and its analogues as leads toward development of anti-ovarian cancer agents.

Virginia Commonwealth University

Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

Virginia Commonwealth University

14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.

Virginia Commonwealth University

Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.

Virginia Commonwealth University

Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.

Virginia Commonwealth University

Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.

Virginia Commonwealth University

1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.

Virginia Commonwealth University

Interaction of chiral MS-245 analogs at h5-HT6 receptors.

Virginia Commonwealth University

Possible differences in modes of agonist and antagonist binding at human 5-HT6 receptors.

Virginia Commonwealth University

Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).

Virginia Commonwealth University

Ketanserin analogues: the effect of structural modification on 5-HT2 serotonin receptor binding.

Virginia Commonwealth University

Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.

Virginia Commonwealth University

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.

Virginia Commonwealth University

Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.

Virginia Commonwealth University

Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.

Virginia Commonwealth University

Identification and exploitation of the sigma-opiate pharmacophore.

Virginia Commonwealth University

Muscarinic receptor binding profile of para-substituted caramiphen analogues.

Virginia Commonwealth University

Design and synthesis of propranolol analogues as serotonergic agents.

Virginia Commonwealth University

1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.

Virginia Commonwealth University

(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

Virginia Commonwealth University

Exploring new non-sugar sulfated molecules as activators of antithrombin.

Virginia Commonwealth University

Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.

Virginia Commonwealth University

The natural product CCR5 antagonist anibamine and its analogs as anti-prostate cancer agents.

Virginia Commonwealth University

Rational design of potent, small, synthetic allosteric inhibitors of thrombin.

Virginia Commonwealth University

9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.

Virginia Commonwealth University

Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.

Virginia Commonwealth University

Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.

Virginia Commonwealth University

Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.

Virginia Commonwealth University

Designing Smaller, Synthetic, Functional Mimetics of Sulfated Glycosaminoglycans as Allosteric Modulators of Coagulation Factors.

Virginia Commonwealth University

Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors.

Virginia Commonwealth University

Structural Alterations of the "Address" Moiety of NAN Leading to the Discovery of a Novel Opioid Receptor Modulator with Reduced hERG Toxicity.

Virginia Commonwealth University

Studies on fragment-based design of allosteric inhibitors of human factor XIa.

Virginia Commonwealth University

Interaction of N1-unsubstituted and N1-benzenesulfonyltryptamines at h5-HT6 receptors.

Virginia Commonwealth University

Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.

Virginia Commonwealth University

Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors.

Virginia Commonwealth University

Development of sulfonamide-based NLRP3 inhibitors: Further modifications and optimization through structure-activity relationship studies.

Virginia Commonwealth University

Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors.

Virginia Commonwealth University

Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.

Virginia Commonwealth University

Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.

Virginia Commonwealth University

Design, Synthesis, and Biological Evaluation of NAP Isosteres: A Switch from Peripheral to Central Nervous System Acting Mu-Opioid Receptor Antagonists.

Virginia Commonwealth University

Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.

Virginia Commonwealth University

Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.

Virginia Commonwealth University

2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.

Virginia Commonwealth University

Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).

Virginia Commonwealth University

Thioxanthene-derived analogs as sigma(1) receptor ligands.

Virginia Commonwealth University

Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.

Virginia Commonwealth University

Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.

Virginia Commonwealth University

Binding of an imidazopyridoindole at imidazoline I2 receptors.

Virginia Commonwealth University

Binding of beta-carbolines at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.

Virginia Commonwealth University

N1-benzenesulfonylgramine and N1-benzenesulfonylskatole: novel 5-HT6 receptor ligand templates.

Virginia Commonwealth University

Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.

Virginia Commonwealth University

Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.

Virginia Commonwealth University

Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.

Virginia Commonwealth University

Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.

Virginia Commonwealth University

Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization.

Virginia Commonwealth University

Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.

Virginia Commonwealth University

Geometry-affinity relationships of the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.

Virginia Commonwealth University

Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.

Virginia Commonwealth University

1-[2-methoxy-5-(3-phenylpropyl)]-2-aminopropane unexpectedly shows 5-HT(2A) serotonin receptor affinity and antagonist character.

Virginia Commonwealth University

Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.

Virginia Commonwealth University

Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.

Virginia Commonwealth University

Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.

Virginia Commonwealth University

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Virginia Commonwealth University

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists.

Virginia Commonwealth University

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.

Virginia Commonwealth University

Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.

Virginia Commonwealth University

Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.

Virginia Commonwealth University

Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands.

Virginia Commonwealth University

Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.

Virginia Commonwealth University

Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.

Virginia Commonwealth University

Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.

Virginia Commonwealth University

A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.

Virginia Commonwealth University

Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.

Virginia Commonwealth University

Structural features important for sigma 1 receptor binding.

Virginia Commonwealth University

Design, synthesis, and biological evaluation of 14-heteroaromatic-substituted naltrexone derivatives: pharmacological profile switch from mu opioid receptor selectivity to mu/kappa opioid receptor dual selectivity.

Virginia Commonwealth University

Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opioid receptor selective antagonists.

Virginia Commonwealth University

Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors.

Virginia Commonwealth University

Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.

Virginia Commonwealth University

Structure activity relationship studies of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan (NAQ) analogues as potent opioid receptor ligands: preliminary results on the role of electronic characteristics for affinity and function.

Virginia Commonwealth University

Opioid receptor selectivity profile change via isosterism for 14-O-substituted naltrexone derivatives.

Virginia Commonwealth University

Designing allosteric regulators of thrombin. Exosite 2 features multiple subsites that can be targeted by sulfated small molecules for inducing inhibition.

Virginia Commonwealth University

On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.

Virginia Commonwealth University

3-(2-Aminoethyl)pyridine analogs as alpha4beta2 nicotinic cholinergic receptor ligands.

Virginia Commonwealth University

6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand.

Virginia Commonwealth University

Arylpiperazine derivatives as high-affinity 5-HT1A serotonin ligands.

Virginia Commonwealth University

A small group of sulfated benzofurans induces steady-state submaximal inhibition of thrombin.

Virginia Commonwealth University

N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin.

Virginia Commonwealth University

N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites?

Virginia Commonwealth University

2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites.

Virginia Commonwealth University

5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.

Virginia Commonwealth University

Binding of indolylalkylamines at 5-HT2 serotonin receptors: examination of a hydrophobic binding region.

Virginia Commonwealth University

Diaminopimelic acid (DAP) analogs bearing isoxazoline moiety as selective inhibitors against meso-diaminopimelate dehydrogenase (m-Ddh) from Porphyromonas gingivalis.

Virginia Commonwealth University

A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3).

Virginia Commonwealth University

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.

Virginia Commonwealth University

Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.

Virginia Commonwealth University

Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.

Virginia Commonwealth University

Reevaluation of fenpropimorph as aσ receptor ligand: Structure-affinity relationship studies at humanσ

Virginia Commonwealth University

Compounds, compositions, and methods for selectively inhibiting β-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea

Symberix

Inhibitors of soluble adenylyl cyclase

Cornell University

Inhibitors of RPN11

California Institute of Technology

Benzimidazole derivatives as RLK and ITK inhibitors

Principia Biopharma

Inhibitors of bruton's tyrosine kinase

Hoffmann-La Roche

The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons.

Cns-Pharmacology

Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.

University of Sheffield

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists.

Genentech

Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.

Bristol-Myers Squibb

Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.

University of Michigan

Inhibitors of the Diadenosine Tetraphosphate Phosphorylase Rv2613c of Mycobacterium tuberculosis.

University of Konstanz