Cargando…

Structure–Affinity Relationships and Structure–Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists

[Image: see text] We report on the synthesis and biological evaluation of a series of 1,2-diarylimidazol-4-carboxamide derivatives developed as CB(1) receptor antagonists. These were evaluated in a radioligand displacement binding assay, a [(35)S]GTPγS binding assay, and in a competition association...

Descripción completa

Detalles Bibliográficos
Autores principales:	Xia, Lizi, de Vries, Henk, Lenselink, Eelke B., Louvel, Julien, Waring, Michael J., Cheng, Leifeng, Pahlén, Sara, Petersson, Maria J., Schell, Peter, Olsson, Roine I., Heitman, Laura H., Sheppard, Robert J., IJzerman, Adriaan P.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2017
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734604/ https://www.ncbi.nlm.nih.gov/pubmed/29111736 http://dx.doi.org/10.1021/acs.jmedchem.7b00861

Ejemplares similares

Structure–Affinity Relationships and Structure–Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A(3) Receptor Antagonists
por: Xia, Lizi, et al.
Publicado: (2017)

A covalent antagonist for the human adenosine A(2A) receptor
por: Yang, Xue, et al.
Publicado: (2016)

In search of novel ligands using a structure-based approach: a case study on the adenosine A(2A) receptor
por: Lenselink, Eelke B., et al.
Publicado: (2016)

Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides
por: Ugwu, D. I., et al.
Publicado: (2014)

Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics
por: Hothersall, J. Daniel, et al.
Publicado: (2017)

Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A(3) Receptor
por: Yang, Xue, et al.
Publicado: (2019)

Successive Statistical and Structure-Based Modeling to Identify Chemically Novel Kinase Inhibitors
por: Burggraaff, Lindsey, et al.
Publicado: (2020)

Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5
por: Ortiz Zacarías, Natalia V., et al.
Publicado: (2019)

Optimized 4,5-Diarylimidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK
por: Halekotte, Jakob, et al.
Publicado: (2017)

Structure–Effect Relationships of Novel Semi-Synthetic Cannabinoid Derivatives
por: Götz, Marcus R., et al.
Publicado: (2019)

Structure–Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D
por: Mock, Elliot D., et al.
Publicado: (2020)

Beyond the hype: deep neural networks outperform established methods using a ChEMBL bioactivity benchmark set
por: Lenselink, Eelke B., et al.
Publicado: (2017)

New 4,5-Diarylimidazol-2-ylidene–iodidogold(I) Complexes with High Activity against Esophageal Adenocarcinoma Cells
por: Schleser, Sebastian W., et al.
Publicado: (2023)

The Structure–Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation
por: Bow, Eric W., et al.
Publicado: (2016)

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A(3) receptor
por: Bouzo-Lorenzo, Monica, et al.
Publicado: (2019)

Synthesis of Halogenated 1,5-Diarylimidazoles and Their Inhibitory Effects on LPS-Induced PGE(2) Production in RAW 264.7 Cells
por: Yang, Zunhua, et al.
Publicado: (2021)

Three-Dimensional Quantitative Structure-Activity Relationships (3D-QSAR) on a Series of Piperazine-Carboxamides Fatty Acid Amide Hydrolase (FAAH) Inhibitors as a Useful Tool for the Design of New Cannabinoid Ligands
por: Lorca, Marcos, et al.
Publicado: (2019)

Scintillation proximity assay (SPA) as a new approach to determine a ligand’s kinetic profile. A case in point for the adenosine A(1) receptor
por: Xia, Lizi, et al.
Publicado: (2015)

New carboxamide derivatives bearing benzenesulphonamide as a selective COX-II inhibitor: Design, synthesis and structure-activity relationship
por: Ugwu, David Izuchukwu, et al.
Publicado: (2017)

Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2
por: Ortiz Zacarías, Natalia V., et al.
Publicado: (2018)

Multitask machine learning models for predicting lipophilicity (logP) in the SAMPL7 challenge
por: Lenselink, Eelke B., et al.
Publicado: (2021)

Novel Machaeriol Analogues as Modulators of Cannabinoid Receptors: Structure–Activity Relationships of (+)-Hexahydrocannabinoids and Their Isoform Selectivities
por: Haider, Saqlain, et al.
Publicado: (2021)

Crystal structure of benzo[h]quinoline-3-carboxamide
por: Grathwol, Christoph W., et al.
Publicado: (2019)

Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1
por: Vlachodimou, Anna, et al.
Publicado: (2019)

Predicting Binding Affinities for GPCR Ligands Using Free-Energy Perturbation
por: Lenselink, Eelke B., et al.
Publicado: (2016)

Discovery and Structure–Activity Relationship of Novel 2,3-Dihydrobenzofuran-7-carboxamide and 2,3-Dihydrobenzofuran-3(2H)-one-7-carboxamide Derivatives as Poly(ADP-ribose)polymerase-1 Inhibitors
por: Patel, Maulik R., et al.
Publicado: (2014)

Structural basis of selective cannabinoid CB(2) receptor activation
por: Li, Xiaoting, et al.
Publicado: (2023)

A quantitative analysis of microbial community structure-function relationships in plant litter decay
por: Waring, Bonnie, et al.
Publicado: (2022)

Three Dimensional Quantitative Structure-Activity Relationship of 5H-Pyrido[4,3-b]indol-4-carboxamide JAK2 Inhibitors
por: Wu, Xiaoyun, et al.
Publicado: (2013)

Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
por: Khurana, Leepakshi, et al.
Publicado: (2014)

Evaluation of carboxamide-type synthetic cannabinoids as CB(1)/CB(2) receptor agonists: difference between the enantiomers
por: Doi, Takahiro, et al.
Publicado: (2017)

Inhibitory Effect of AB-PINACA, Indazole Carboxamide Synthetic Cannabinoid, on Human Major Drug-Metabolizing Enzymes and Transporters
por: Park, Eun Jeong, et al.
Publicado: (2020)

Crystal structures of three 6-substituted coumarin-3-carboxamide derivatives
por: Gomes, Lígia R., et al.
Publicado: (2016)

Crystal structure of N-hydroxyquinoline-2-carboxamide monohydrate
por: Safyanova, Inna S., et al.
Publicado: (2017)

Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors
por: Yang, Man, et al.
Publicado: (2022)

Discovery and Structure–Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2′-Oxidase
por: Oh, Sangmi, et al.
Publicado: (2018)

Antitumor Cannabinoid Chemotypes: Structural Insights
por: Morales, Paula, et al.
Publicado: (2019)

Does Gender Matter in the Relationship between Anxiety and Decision-Making?
por: Zhang, Fenghua, et al.
Publicado: (2017)

Cannabinoid Receptors and Their Relationship With Chronic Pain: A Narrative Review
por: Anthony, Adarsh Thomas, et al.
Publicado: (2020)

Structure–Activity Relationship Development Efforts towards Peripherally Selective Analogs of the Cannabinoid Receptor Partial Agonist BAY 59-3074
por: Amato, George, et al.
Publicado: (2022)

Cannot write session to /tmp/vufind_sessions/sess_37v64e7c0q6ltirr7dd1l67th8