PMID

Data

Article Title

Organization

Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.

Mayo Clinic

Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.

Glaxosmithkline

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

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)

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

Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.

Rochester

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

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

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

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

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

Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.

TBA

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

 

Pseudopeptide CCK-4 analogues incorporating the [CH(CN)NH] peptide bond surrogate

TBA

 

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

 

Biological properties of (R)-4-benzamido-5-oxopentanoic basic derivatives as CCK-antagonists

TBA

New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R).

University of Trieste

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

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

 

Design and synthesis of novel nonpeptide CCK-B receptor antagonists

TBA

 

Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines

TBA

 

SAR study of the indole moiety of CI-988, a potent and selective CCK-B antagonist

TBA

 

CCK-4 restricted analogues containing a 3-oxoindolizidine skeleton

TBA

 

Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022

TBA

 

Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

TBA

 

C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCK_B/gastrin receptor antagonists

TBA

 

CCK_B selective receptor ligands: novel 1,3,5-trisubstituted benzazepin-2-ones

TBA

 

Alternative strategies towards the identification of chemical lead compounds by rational design

TBA

 

Methionine replacements in biologically active peptides

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

 

Benzolactams as non-peptide cholecystokinin receptor ligands

TBA

 

Multipurpose receptor ligands: β-carboline cholecystokinin antagonists

TBA

 

Diastereoselective synthesis of cyclopropyl phenylalanines and their incorporation into dipeptides

TBA

 

Synthesis and sar study of novel CCK-B antagonists

TBA

 

L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCK_B/gastrin receptor

TBA

 

The use of a proline ring as a conformational restraint in CCK-B receptor “dipeptoids”.

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

Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies.

Lucknow University

Novel benzodiazepine photoaffinity probe stereoselectively labels a site deep within the membrane-spanning domain of the cholecystokinin receptor.

Mayo Clinic

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)

Effects of the incorporation of IBTM beta-turn mimetics into the dipeptoid CCK(1) receptor agonist PD 170292.

Instituto De QuíMica MéDica (Csic)

Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.

Instituto De QuíMica MéDica (Csic)

Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.

Fujisawa Pharmaceutical

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

(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

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

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

Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.

Glaxo Wellcome Medicines Research Centre

Synthesis and biological activity of new peptide segments of gastrin exhibiting gastrin antagonist property.

TBA

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

Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.

TBA

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

Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.

Center For Bio-Pharmaceutical Sciences

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