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Substituted Purines as High-Affinity Histamine H3 Receptor Ligands

https://doi.org/10.3390/ph15050573
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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

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Multitarget‐Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases
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A BOILED‐Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small Molecules
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The VSGB 2.0 model: A next generation energy model for high resolution protein structure modeling
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Role of the Histamine H3 Receptor in the Central Nervous System
inferredcites →https://doi.org/10.1007/s10822-013-9644-8openalex-snapshot
Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments
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Pitolisant: A Review in Narcolepsy with or without Cataplexy
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Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
inferredcites →https://doi.org/10.1016/j.bioorg.2019.103361openalex-snapshot
New 2,6,9-trisubstituted purine derivatives as Bcr-Abl and Btk inhibitors and as promising agents against leukemia
inferredcites →https://doi.org/10.1016/j.bmc.2005.12.060openalex-snapshot
The purines: Potent and versatile small molecule inhibitors and modulators of key biological targets
inferredcites →https://doi.org/10.1016/j.bmc.2019.05.042openalex-snapshot
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H3 receptor
inferredcites →https://doi.org/10.1016/j.bmcl.2013.02.118openalex-snapshot
Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
inferredcites →https://doi.org/10.1016/j.bmcl.2018.07.023openalex-snapshot
New lead elements for histamine H3 receptor ligands in the pyrrolo[2,3-d]pyrimidine class
inferredcites →https://doi.org/10.1016/j.bmcl.2019.04.015openalex-snapshot
Synthesis and evaluation of histamine H3 receptor ligand based on lactam scaffold as agents for treating neuropathic pain
inferredcites →https://doi.org/10.1016/j.ddtec.2013.07.001openalex-snapshot
Scaffold variations in amine warhead of histamine H3 receptor antagonists
inferredcites →https://doi.org/10.1016/j.ejmech.2016.02.018openalex-snapshot
Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors
inferredcites →https://doi.org/10.1016/j.pharmthera.2019.04.007openalex-snapshot
Histamine H3 receptor antagonists/inverse agonists: Where do they go?
inferredcites →https://doi.org/10.1016/s0169-409x(00)00129-0openalex-snapshot
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings 1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997) 3–25. 1
inferredcites →https://doi.org/10.1021/acs.jctc.1c00302openalex-snapshot
OPLS4: Improving Force Field Accuracy on Challenging Regimes of Chemical Space
inferredcites →https://doi.org/10.1021/acs.jmedchem.9b01462openalex-snapshot
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity
inferredcites →https://doi.org/10.1021/ci100031xopenalex-snapshot
Conformer Generation with OMEGA: Algorithm and Validation Using High Quality Structures from the Protein Databank and Cambridge Structural Database
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Molecular Properties That Influence the Oral Bioavailability of Drug Candidates
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Synthesis, Biological Activity, and SAR of Antimycobacterial 9-Aryl-, 9-Arylsulfonyl-, and 9-Benzyl-6-(2-furyl)purines
inferredcites →https://doi.org/10.1021/jm050540copenalex-snapshot
Novel Procedure for Modeling Ligand/Receptor Induced Fit Effects
inferredcites →https://doi.org/10.1038/nature10236openalex-snapshot
Structure of the human histamine H1 receptor complex with doxepin
inferredcites →https://doi.org/10.1038/srep42717openalex-snapshot
SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules
inferredcites →https://doi.org/10.1080/14756366.2018.1509212openalex-snapshot
Design, synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists
inferredcites →https://doi.org/10.1093/nar/gkaa1080openalex-snapshot
GPCRdb in 2021: integrating GPCR sequence, structure and function
inferredcites →https://doi.org/10.1093/nar/gkr703openalex-snapshot
OPM database and PPM web server: resources for positioning of proteins in membranes
inferredcites →https://doi.org/10.1093/nar/gkv1178openalex-snapshot
GPCRdb: an information system for G protein-coupled receptors
inferredcites →https://doi.org/10.1093/nar/gkx1109openalex-snapshot
GPCRdb in 2018: adding GPCR structure models and ligands
inferredcites →https://doi.org/10.1111/j.1747-0285.2005.00327.xopenalex-snapshot
Use of an Induced Fit Receptor Structure in Virtual Screening
inferredcites →https://doi.org/10.1111/j.1755-5949.2010.00212.xopenalex-snapshot
Histamine Pharmacology and New CNS Drug Targets
inferredcites →https://doi.org/10.1124/pr.114.010249openalex-snapshot
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
inferredcites →https://doi.org/10.1126/science.281.5376.533openalex-snapshot
Exploiting Chemical Libraries, Structure, and Genomics in the Search for Kinase Inhibitors
inferredcites →https://doi.org/10.1159/000444256openalex-snapshot
Modulating Innate and Adaptive Immunity by (R)-Roscovitine: Potential Therapeutic Opportunity in Cystic Fibrosis
inferredcites →https://doi.org/10.1248/cpb.58.1353openalex-snapshot
Kojic Acid Derivatives as Histamine H3 Receptor Ligands
inferredcites →https://doi.org/10.1517/14728220903188438openalex-snapshot
Histamine H3and H4receptors as novel drug targets
inferredcites →https://doi.org/10.2174/0929867325666171123203550openalex-snapshot
Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives
inferredcites →https://doi.org/10.2174/138955709789957440openalex-snapshot
8-Azapurine Nucleus: A Versatile Scaffold for Different Targets
inferredcites →https://doi.org/10.3390/ijms22168372openalex-snapshot
A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo
inferredcites →https://doi.org/10.3390/molecules26061778openalex-snapshot
Molecular Modeling of Histamine Receptors—Recent Advances in Drug Discovery

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

inferred← citeshttps://doi.org/10.2139/ssrn.4489243openalex-extracted
Synthesis of Purine Conjugates with Bis-Carboranyl Derivatives of (S)-Lysine or (S)-Glutamic Acid
inferred← citeshttps://doi.org/10.2139/ssrn.4496950openalex-extracted
Synthesis of Purine Conjugates with Bis-Carboranyl Derivatives of (S)-Lysine or (S)-Glutamic Acid
inferred← citeshttps://doi.org/10.1002/ardp.202400387openalex-snapshot
First in class pyrrolo[2,3‐d]pyrimidine derivatives fused to fluorobenzylpiperidines as dual ligands of acetylcholinesterase and histamine H3 receptor
inferred← citeshttps://doi.org/10.1007/s11064-025-04521-9openalex-snapshot
Histamine H3 Receptor Antagonists Influence the Directional Growth of Type II Spiral Ganglion Neurites Within the Developing Cochlea of C57BL/6 Mice
inferred← citeshttps://doi.org/10.1016/j.tetlet.2023.154686openalex-snapshot
Synthesis of purine conjugates with bis-carboranyl derivatives of (S)-lysine or (S)-glutamic acid
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