Oxetanes in drug discovery: structural and synthetic insights.
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Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in VivoDiscovery of ML326: The first sub-micromolar, selective M5 PAMExploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinIdentification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, SDiscovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.Oxetanyl peptides: novel peptidomimetic modules for medicinal chemistry.A bifunctional dimethylsulfoxide substitute enhances the aqueous solubility of small organic molecules.Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.2-(Aryl-sulfonyl)oxetanes as designer 3-dimensional fragments for fragment screening: synthesis and strategies for functionalisation.Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice.Structurally Divergent Lithium Catalyzed Friedel-Crafts Reactions on Oxetan-3-ols: Synthesis of 3,3-Diaryloxetanes and 2,3-DihydrobenzofuransBradykinin B1 receptor antagonists: a patent update 2009 - 2012.A compendium of cyclic sugar amino acids and their carbocyclic and heterocyclic nitrogen analogues.Asymmetric synthesis of 2-substituted oxetan-3-ones via metalated SAMP/RAMP hydrazones.Molecular recognition in chemical and biological systems.Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.2-(3-{(3R,4R)-4-Methyl-3-[meth-yl(7H-pyrrolo-[2,3-d]pyrimidin-4-yl)amino]-piperidin-1-yl}oxetan-3-yl)aceto-nitrile monohydrate.Tyrosine kinase inhibitor Thiotanib targets Bcr-Abl and induces apoptosis and autophagy in human chronic myeloid leukemia cells.Catalytic asymmetric nucleophilic openings of 3-substituted oxetanes.Square sugars: challenges and synthetic strategies.Single-step microwave-mediated synthesis of oxazoles and thiazoles from 3-oxetanone: a synthetic and computational study.Metabolically Stable tert-Butyl ReplacementInvestigating the Influence of (Deoxy)fluorination on the Lipophilicity of Non-UV-Active Fluorinated Alkanols and Carbohydrates by a New log P Determination Method.Studies on the synthesis, stability and conformation of 2-sulfonyl-oxetane fragments.Synthesis of di-, tri-, and tetrasubstituted oxetanes by rhodium-catalyzed O-H insertion and C-C bond-forming cyclizationSite-Selective Modification of Proteins with Oxetanes.An uncharged oxetanyl sulfoxide as a covalent modifier for improving aqueous solubility.Catalytic enantioselective intermolecular desymmetrization of 3-substituted oxetanes.Discovery of a Novel Microsomal Epoxide Hydrolase-Catalyzed Hydration of a Spiro Oxetane.Design and synthesis of tricyclic JAK3 inhibitors with picomolar affinities as novel molecular probes.A Direct Synthesis of Highly Substituted π-Rich Aromatic Heterocycles from Oxetanes.Complex bioactive alkaloid-type polycycles through efficient catalytic asymmetric multicomponent aza-Diels-Alder reaction of indoles with oxetane as directing group.Highly regioselective lithiation of pyridines bearing an oxetane unit by n-butyllithium.Efficient endo Cycloisomerization of Terminal Alkynols Catalyzed by a New Ruthenium Complex with 8-(Diphenylphosphino)quinoline Ligand and Mechanistic Investigation.Effect of Partially Fluorinated N-Alkyl-Substituted Piperidine-2-carboxamides on Pharmacologically Relevant Properties.Trifluoromethyl Oxetanes: Synthesis and Evaluation as a tert-Butyl Isostere.Lithium-Catalyzed Thiol Alkylation with Tertiary and Secondary Alcohols: Synthesis of 3-Sulfanyl-Oxetanes as Bioisosteres.C-H Insertion as a Key Step to Spiro-Oxetanes, Scaffolds for Drug Discovery.Stereoselective synthesis of 2,3,4-highly substituted oxetanes by intramolecular C-C bond forming Michael addition.
P2860
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P2860
Oxetanes in drug discovery: structural and synthetic insights.
description
2010 nî lūn-bûn
@nan
2010年の論文
@ja
2010年学术文章
@wuu
2010年学术文章
@zh
2010年学术文章
@zh-cn
2010年学术文章
@zh-hans
2010年学术文章
@zh-my
2010年学术文章
@zh-sg
2010年學術文章
@yue
2010年學術文章
@zh-hant
name
Oxetanes in drug discovery: structural and synthetic insights.
@en
Oxetanes in drug discovery: structural and synthetic insights.
@nl
type
label
Oxetanes in drug discovery: structural and synthetic insights.
@en
Oxetanes in drug discovery: structural and synthetic insights.
@nl
prefLabel
Oxetanes in drug discovery: structural and synthetic insights.
@en
Oxetanes in drug discovery: structural and synthetic insights.
@nl
P2093
P356
P1476
Oxetanes in drug discovery: structural and synthetic insights.
@en
P2093
Björn Wagner
Franz Schuler
Georg Wuitschik
Holger Fischer
Isabelle Parrilla
Klaus Müller
Mark Rogers-Evans
P304
P356
10.1021/JM9018788
P407
P577
2010-04-01T00:00:00Z