CNS drug design: balancing physicochemical properties for optimal brain exposure.
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Drug Design for CNS Diseases: Polypharmacological Profiling of Compounds Using Cheminformatic, 3D-QSAR and Virtual Screening MethodologiesA Role for Fragment-Based Drug Design in Developing Novel Lead Compounds for Central Nervous System TargetsMolecular determinants of blood-brain barrier permeationA BOILED-Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small MoleculesEfficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain.Tertiary Amine Pyrazolones and Their Salts as Inhibitors of Mutant Superoxide Dismutase 1-Dependent Protein Aggregation for the Treatment of Amyotrophic Lateral Sclerosis.Development of an in-vivo active reversible butyrylcholinesterase inhibitor.Design, synthesis and multitarget biological profiling of second-generation anti-Alzheimer rhein-huprine hybrids.Validation of an immortalized human (hBMEC) in vitro blood-brain barrier model.Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.A High-Throughput Screen to Identify LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease Using RapidFire Mass Spectrometry.Analysis of Cancer-Targeting Alkylphosphocholine Analogue Permeability Characteristics Using a Human Induced Pluripotent Stem Cell Blood-Brain Barrier Model.Tactics for preclinical validation of receptor-binding radiotracers.Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Asymmetric synthesis and in vitro and in vivo activity of tetrahydroquinolines featuring a diverse set of polar substitutions at the 6 position as mixed-efficacy μ opioid receptor/δ opioid receptor ligands.Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.Synthesis and opioid receptor binding of indium (III) and [111In]-labeled macrocyclic conjugates of diprenorphine: novel ligands designed for imaging studies of peripheral opioid receptors.Probabilistic Approach to Generating MPOs and Its Application as a Scoring Function for CNS Drugs.Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.Synthesis and Evaluation of Orexin-1 Receptor Antagonists with Improved Solubility and CNS Permeability.Synthesis and Determination of Lipophilicity, Anticonvulsant Activity, and Preliminary Safety of 3-Substituted and 3-Unsubstituted N-[(4-Arylpiperazin-1-yl)alkyl]pyrrolidine-2,5-dione Derivatives.Challenges of developing small molecule kinase inhibitors for brain tumors and the need for emphasis on free drug levels.A Small-Molecule Inhibitor of Prion Replication and Mutant Prion Protein Toxicity.Chances and challenges of retinoid X receptor gamma targeting for regenerative multiple sclerosis treatment.Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.Assessment of the classification abilities of the CNS multi-parametric optimization approach by the method of logistic regression.Physicochemical property profile for brain permeability: comparative study by different approaches.Identification of ion-channel modulators that protect against aminoglycoside-induced hair cell death.A perspective on multi-target drug discovery and design for complex diseases.Brain distribution of a novel MEK inhibitor E6201: implications in the treatment of melanoma brain metastases.Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.CNS Multiparameter Optimization Approach: Is it in Accordance with Occam's Razor Principle?A Versatile Approach to CF3 -Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amidine Class BACE1 Inhibitors.Small-Molecule Inhibitors of LRRK2.RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345.MetStabOn-Online Platform for Metabolic Stability Predictions.Current Challenges and Opportunities in Treating Glioblastoma.Syntheses and in vitro evaluation of new S1PR1 compounds and initial evaluation of a lead F-18 radiotracer in rodents.Modular synthesis of thirty lead-like scaffolds suitable for CNS drug discovery.Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742.
P2860
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P2860
CNS drug design: balancing physicochemical properties for optimal brain exposure.
description
2015 nî lūn-bûn
@nan
2015年の論文
@ja
2015年論文
@yue
2015年論文
@zh-hant
2015年論文
@zh-hk
2015年論文
@zh-mo
2015年論文
@zh-tw
2015年论文
@wuu
2015年论文
@zh
2015年论文
@zh-cn
name
CNS drug design: balancing physicochemical properties for optimal brain exposure.
@en
type
label
CNS drug design: balancing physicochemical properties for optimal brain exposure.
@en
prefLabel
CNS drug design: balancing physicochemical properties for optimal brain exposure.
@en
P356
P1476
CNS drug design: balancing physicochemical properties for optimal brain exposure.
@en
P2093
Zoran Rankovic
P304
P356
10.1021/JM501535R
P407
P577
2015-01-06T00:00:00Z