125 articles for AP Kozikowski
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Article Title
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Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.
University of Illinois At Chicago
Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.
University of Illinois At Chicago
Synthesis and biological evaluation of novel hybrids of highly potent and selectivea4ß2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
University of Illinois At Chicago
Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51.
University of Illinois At Chicago
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University of Illinois At Chicago
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
University of Illinois At Chicago
Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors.
University of Illinois At Chicago
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selectivea4ß2-nAChR Ligands.
University of Illinois At Chicago
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
University of Illinois At Chicago
Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selectivea4ß2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.
University of Illinois At Chicago
Structural analogs of huperzine A improve survival in guinea pigs exposed to soman.
University of Illinois At Chicago
An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity.
University of Chicago
Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) asa4ß2-nicotinic acetylcholine receptor-selective partial agonists.
University of Illinois At Chicago
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
Discovery of highly potent and selectivea4ß2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.
University of Illinois At Chicago
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.
University of Illinois At Chicago
Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands toa4ß2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands.
University of Illinois At Chicago
Identification of novela4ß2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
University of Illinois At Chicago
Chemistry and behavioral studies identify chiral cyclopropanes as selectivea4ß2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.
University of Illinois At Chicago
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.
TBA
Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells.
University of Illinois At Chicago
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.
University of Illinois At Chicago
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.
University of Messina
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Acenta Discovery
Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring.
University of Illinois At Chicago
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.
Georgetown University Medical Center
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors.
Georgetown University Medical Center
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.
Georgetown University Medical Center
Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors.
Georgetown University Medical Center
Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors.
Georgetown University Medical Center
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.
Georgetown University Medical Center
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.
Georgetown University Medical Center
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.
Georgetown University Medical Center
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.
Georgetown University Medical Center
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
Georgetown University Medical Center
Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position.
Mayo Foundation
The novel Ins(1,4,5)P3 analogue 3-amino-3-deoxy-Ins(1,4,5)P3: a pH-dependent Ins(1,4,5)P3 receptor partial agonist in SH-SY5Y neuroblastoma cells.
Mayo Foundation
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding.
Trophix Pharmaceuticals
Deoxygenated inositol 1,4,5-trisphosphate analogues and their interaction with metabolic enzymes. (1R,2R,4R)-cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor.
Mayo Foundation
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.
Mayo Foundation
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity.
Mayo Clinic
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Georgetown University Medical Center
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Georgetown University Medical Center
Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B.
Georgetown University Medical Center
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.
Georgetown University Medical Center
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.
Georgetown University Medical Center
Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors.
Georgetown University Medical Center
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.
Georgetown University Medical Center
Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A.
Georgetown University Medical Center
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.
Georgetown University Medical Center
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.
Georgetown University Medical Center
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.
Georgetown University Medical Center
Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.
Georgetown University Medical Center
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.
Georgetown University Medical Center
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.
Georgetown University Medical Center
Synthesis of ()-10,10-dimethylhuperzine A a huperzine analogue possessing a slower enzyme off-rate
TBA
SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency
TBA
Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.
University of Illinois At Chicago
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
Walter Reed Army Institute of Research
Identification and development of novel inhibitors of Toxoplasma gondii enoyl reductase.
University of Illinois At Chicago
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
University of Illinois At Chicago
Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-an apparent mGluR6 selective ligand
TBA
Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA)
TBA
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
TBA
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.
TBA
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
University of Illinois At Chicago
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
University of Illinois At Chicago
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
University of Illinois At Chicago
A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer.
Molecular Insight Pharmaceuticals
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.
University of Illinois At Chicago
Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase.
University of Illinois At Chicago
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
University of Illinois At Chicago
Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A.
University of Illinois at Chicago
Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies.
University of Illinois At Chicago
Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors.
Scripps Research
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
University of Illinois At Chicago
Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors.
University of Illinois At Chicago
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Acenta Discovery
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
University of Illinois At Chicago
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
University of Illinois At Chicago
Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.
University of Illinois At Chicago
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
University of Illinois At Chicago
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Georgetown University Medical Center
Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.
The George Washington University
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.
Georgetown University Medical Center
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
University of Illinois At Chicago
Structural basis of RasGRP binding to high-affinity PKC ligands.
Georgetown University Medical Center
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
TBA
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
Georgetotwn University
Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor.
University of Illinois At Chicago
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Institute of Organic Chemistry
3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth.
Georgetown University Medical Center
A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents.
Georgetown University Medical Center
Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection.
Chicago State University
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.
Georgetown University Medical Center
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationships, and behavioral pharmacological studies.
Georgetown University Medical Center
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
Shanghaitech University
Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
Georgetown University Medical Center
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.
Georgetown University Medical Center
Synthesis and protein kinase C binding activity of benzolactam-V7.
Institute of Organic Chemistry
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
University of Illinois At Chicago
alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.
Georgetown University Medical Center
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
University of Illinois At Chicago
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.
Georgetown University Medical Center
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.
University of Pennsylvania
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Georgetown University Medical Center
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Mayo Foundation
Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis.
University of Illinois At Chicago
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
University of Illinois At Chicago
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Georgetown University Medical Center
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth.
Georgetown University Medical Center
2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.
University of Illinois At Chicago
Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.
University of Illinois At Chicago
Characterisation of hydrazides and hydrazine derivatives as novel aspartic protease inhibitors.
University of Karachi
Optically active pyrazolylaminoquinazoline, and pharmaceutical compositions and methods of use thereof
Ambit Biosciences
A general strategy for creating "inactive-conformation" abl inhibitors.
The Scripps Research Institute
Benzobis(imidazolium)-cucurbit[8]uril complexes for binding and sensing aromatic compounds in aqueous solution.
University of Cambridge
Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Methylgene