179 articles for thisTarget
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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.
Mayo Clinic
Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.
Mayo Clinic
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
Glaxo Wellcome Research and Development
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist"trigger".
Glaxo Wellcome
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
Glaxo Wellcome Research and Development
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
Glaxo Research Institute
Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.
Glaxosmithkline
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.
Johnson & Johnson Pharmaceutical Research and Development
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Mayo Clinic
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
James Black Foundation
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Glaxo Wellcome Research and Development
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
Glaxo Research Institute
Three-dimensional molecular shape analysis-quantitative structure-activity relationship of a series of cholecystokinin-A receptor antagonists.
University of Illinois At Chicago
Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
Pfizer
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University of Arizona
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Abbott Laboratories
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University of Arizona
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
Instituto De Qu£Mica M£Dica (Csic)
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.
Instituto De Qu£Mica M£Dica (Csic)
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.
Instituto De Qu£Mica M£Dica (Csic)
beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
Instituto De Qu£Mica M£Dica (Csic)
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.
James Black Foundation
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
Astrazeneca R&D Boston
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
Insituto De Qu�Mica M�Dica (Csic)
Second generation"peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Warner-Lambert
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
University of Paris
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
Rochester
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University of Arizona
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
Rotta Research Laboratorium
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
Merck Sharp and Dohme Research Laboratories
Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.
Abbott Laboratories
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
Abbott Laboratories
CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Abbott Laboratories
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and"mixed" CCK-A/CCK-B antagonists.
Parke-Davis Neuroscience Research Centre
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Merck Research Laboratories
CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.
University of Paris
Amide bond replacements incorporated into CCK-B selective"dipeptoids".
Parke-Davis Neuroscience Research Center
Rationally designed"dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
Parke-Davis Neuroscience Research Centre
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.
Abbott Laboratories
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
Rotta Research Laboratorium
Rationally designed"dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
Parke-Davis Research Unit
Novel glutamic acid derived cholecystokinin receptor ligands.
Merck Sharp & Dohme Research Laboratories
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Abbott Laboratories
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.
Merck Sharp & Dohme Research Laboratories
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Merck Sharp & Dohme Research Laboratories
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
University of Paris
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
Ccipe-Faculte De Pharmacie
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.
Neurogen
Conversion of acyclic nonpeptide CCK antagonists into CCK agonists
Glaxo Wellcome Research and Development
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
TBA
Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists
TBA
Synthesis of novel iodinated radioligands with high affinity and selectivity for CCK-B/gastrin receptors
TBA
The rational design and synthesis of non-peptide rhegnylogues of CCK-26-33 - a novel series of CCK-A selective ligands
TBA
Synthesis of a potent and selective non-peptide CCK-B/gastrin receptor antagonist tritiated ligand.
TBA
Cholecystokinin analogues: The ergopeptine alkaloids as models of the active conformation of CCK
TBA
New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R).
University of Trieste
Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor.
University Medical Centre Ljubljana
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Merck
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Pfizer
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
2D-QSAR and 3D-QSAR/CoMFA analyses of the N-terminal substituted anthranilic acid based CCK(1) receptor antagonists: 'Hic Rhodus, hic saltus'.
Aristotelian University of Thessaloniki
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Novartis Institutes of Biomedical Research
Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
TBA
Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists
TBA
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
TBA
Alternative strategies towards the identification of chemical lead compounds by rational design
TBA
α-β-didehydrotryptophan as a surrogate for α-methyltryptophan in CCK ‘peptoids’ related to CI-988.
TBA
Selective ligands for cholecystokinin receptor subtypes CCK-A and CCK-B within a single structural class
TBA
Diphenylpyrazolidinone and benzodiazepine cholecystokinin antagonists: A case of convergent evolution in medicinal chemistry
TBA
Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists
TBA
Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics
TBA
Diastereoselective synthesis of cyclopropyl phenylalanines and their incorporation into dipeptides
TBA
Tryptophan-norleucine 1,5-disubstituted tetrazoles as cis peptide bond mimics: Investigation of the bioactive conformation of a potent and selective peptide for the cholecystokinin-B receptor
TBA
L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor
TBA
1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists
TBA
The synthesis and CCK receptor affinities of selected carboyxlic acid mimics of CI-988 - a potent and selective CCK-B antagonist
TBA
Anthranilic acid based CCK1 receptor antagonists: blocking the receptor with the same 'words' of the endogenous ligand.
University of Trieste
2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.
Merck
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Merck Research Laboratories
Recent natural products based drug development: a pharmaceutical industry perspective.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and biological evaluation of cyclic and branched peptide analogues as ligands for cholecystokinin type 1 receptor.
Istituto Di Biostrutture E Bioimmagini-Cnr
Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies.
Lucknow University
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University of Arizona
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their"receptor desmodynamic processes".
University of Naples Federico Ii
Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor.
Mayo Clinic
Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents.
Jiangsu Normal University
Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.
Instituto De QuíMica MéDica (Csic)
Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.
Instituto De QuíMica MéDica (Csic)
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.
St. John'S University
Effects of the incorporation of IBTM beta-turn mimetics into the dipeptoid CCK(1) receptor agonist PD 170292.
Instituto De QuíMica MéDica (Csic)
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
University of Paris
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
Academy of Scientific and Innovative Research (Acsir)
Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.
Instituto De QuíMica MéDica (Csic)
Pharmacological treatment of obesity: therapeutic strategies.
The R. W. Johnson Pharmaceutical Research Institute
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
TBA
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.
Fujisawa Pharmaceutical
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.
University of Paris
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.
Parke-Davis Pharmaceutical Research
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
Instituto De QuíMica MéDica (Csic)
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.
Merck Sharp & Dohme Research Laboratories
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.
Abbott Laboratories
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
Ferring Research Institute
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Neuroscience Research Centre
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties.
University of Paris
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists.
Abbott Laboratories
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
Merck Research Laboratories
Ac-[3- and 4-alkylthioproline31]-CCK4 analogs: synthesis and implications for the CCK-B receptor-bound conformation.
Washington University
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Johnson & Johnson Pharmaceutical Research and Development
Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points.
James Black Foundation
Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands.
Johnson & Johnson Pharmaceutical Research and Development
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
James Black Foundation
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
Glaxo Wellcome Medicines Research Centre
Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons.
James Black Foundation
Improving the affinity and selectivity of a nonpeptide series of cholecystokinin-B/gastrin receptor antagonists based on the dibenzobicyclo[2.2.2]octane skeleton.
James Black Foundation
Synthesis and biological activity of new peptide segments of gastrin exhibiting gastrin antagonist property.
TBA
A new class of non-peptidic cholecystokinin-B/gastrin receptor antagonists based on dibenzobicyclo[2.2.2]octane.
James Black Foundation
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
Merck Sharp & Dohme Research Laboratories
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
University of Paris
Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists.
Abbott Laboratories
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
University of Paris
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
TBA
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Merck Sharp & Dohme Research Laboratories
Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogues.
Roche Research Center
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Abbott Laboratories
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
Abbott Laboratories
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Abbott Laboratories
Boc-Trp-Orn(Z)-Asp-NH2 and derivatives: a new family of CCK antagonists.
University of Paris
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
Center For Bio-Pharmaceutical Sciences
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Abbott Laboratories
N-methylated analogs of Ac[Nle28,31]CCK(26-33): synthesis, activity, and receptor selectivity.
Hadassah-University Hospital
Analogs of CCK incorporating conformationally constrained replacements for Asp32.
Roche Research Center
Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29.
Roche Research Center
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Wyeth Research