Research graph
References from Synthesis, Evaluation, and Context for Applications of SF5-Containing [1.1.1]Bicyclopentane and [ <i>2</i> ]Staffane “Hybrid Bioisosteres”. Local targets link to admitted publications; unresolved targets remain external evidence.
Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design
10.1021/jm1013693 · 2011 · External reference
Expanding the Repertoire of Low-Molecular-Weight Pentafluorosulfanyl-Substituted Scaffolds
10.1002/cmdc.202100641 · 2022 · External reference
Conquering the Synthesis and Functionalization of Bicyclo[1.1.1]pentanes
10.1021/jacsau.3c00014 · 2023 · External reference
Three-Dimensional Saturated C(sp3)-rich Bioisosteres for Benzene
10.1038/s41570-024-00623-0 · 2024 · External reference
Propellane-free Access to Bicyclo[1.1.1]pentanes
10.1038/s41467-026-68309-3 · 2026 · External reference
Strain-Release Pentafluorosulfanylation and Tetrafluoro(aryl)sulfanylation of [1.1.1]Propellane: Reactivity and Structural Insight
10.1002/anie.202211892 · 2022 · External reference
New and Convenient Method for Incorporation of Pentafluorosulfanyl (SF5) Substituents Into Aliphatic Organic Compounds
10.1021/ol026483o · 2002 · External reference
Making the SF5 Group More Accessible: A Gas-Reagent-Free Approach to Aryl Tetrafluoro-λ6-sulfanyl Chlorides
10.1002/anie.201812356 · 2019 · External reference
Unresolved reference
External reference
Amine–Borane Complex-Initiated SF5Cl Radical Addition on Alkenes and Alkynes
10.3762/bjoc.16.256 · 2020 · External reference
Electron Donor–Acceptor (EDA)-Complex Enabled SF5Cl Addition on Alkenes and Alkynes
10.1016/j.jfluchem.2021.109734 · 2021 · External reference
Chemoselective Hydro(Chloro)pentafluorosulfanylation of Diazo Compounds with Pentafluorosulfanyl Chloride
10.1002/anie.202103606 · 2021 · External reference
Radical 1,5-Chloropentafluorosulfanylation of Unactivated Vinylcyclopropanes and Transformation into α-SF5 Ketones
10.1021/acs.joc.1c01886 · 2021 · External reference
Radical Addition of SF5Cl to Cyclopropenes: Synthesis of (Pentafluorosulfanyl)cyclopropanes
10.1021/acs.orglett.1c01840 · 2021 · External reference
Oxidative Fluorination of Heteroatoms Enabled by Trichloroisocyanuric Acid and Potassium Fluoride
10.1002/anie.202205088 · 2022 · External reference
Metal-Free SF6 Activation: A New SF5-Based Reagent Enables Deoxyfluorination and Pentafluorosulfanylation Reactions
10.1002/anie.202204623 · 2022 · External reference
Synthesis and Further Use of SF5-Alkynes as Platforms for the Design of More Complex SF5-Containing Products
10.1016/j.tet.2022.132814 · 2022 · External reference
Photoinitiated Anti-Hydropentafluorosulfanylation of Terminal Alkynes
10.1002/anie.202112575 · 2022 · External reference
Chemistry of Pentafluorosulfanyl Derivatives and Related Analogs: From Synthesis to Applications
10.1002/chem.202201491 · 2022 · External reference
Three-Component Reaction of Pentafluorosulfanyl Chloride, Alkenes and Diazo Compounds and Synthesis of Pentafluorosulfanylfurans
10.1002/anie.202208860 · 2022 · External reference
Light-Activation of SF5Cl for the Atom Transfer Radical Addition onto Alkenes and Alkynes
10.1016/j.jfluchem.2023.110131 · 2023 · External reference
An Extrusion Strategy for On-Demand SF5Cl Gas Generation from a Commercial Disulfide
10.1021/acs.orglett.3c03886 · 2023 · External reference
Tracking SF5I in the Iodopentafluorosulfanylation of Alkynes
10.1002/chem.202302914 · 2023 · External reference
Rhodium-Catalyzed Intramolecular Cyclopropanation of Trifluoromethyl- and Pentafluorosulfanyl-Substituted Allylic Cyanodiazoacetates
10.1021/acs.orglett.3c00642 · 2023 · External reference
Regio- and Stereoselective Hydroelementation of SF5-Alkynes and Further Functionalizations
10.1002/anie.202300685 · 2023 · External reference
Photo-Induced Hydroxypentafluorosulfanylation of Alkenes with SF5Cl and Oxygen Gas and Their Further Derivatization
10.1038/s41467-024-54015-5 · 2024 · External reference
Expanding Radical Chloropentafluorosulfanylation of Alkynes
10.1021/acs.orglett.3c04043 · 2024 · External reference
Pentafluorosulfanylation of Acrylamides: The Synthesis of SF5-Containing Isoquinolinediones with SF5Cl
10.1021/acs.joc.4c02181 · 2024 · External reference
On-Demand Continuous Flow Synthesis of Pentafluorosulfanyl Chloride (SF5Cl) Using a Custom-Made Stirring Packed-Bed Reactor
10.1002/chem.202404039 · 2025 · External reference
Silyl Chloroalkenyl and Alkynyl Sulfur Pentafluorides as Versatile Reagents to Access Novel Fundamental SF5 Building Blocks
10.26434/chemrxiv-2025-jmfh6 · 2025 · External reference
Synthesis of α-SF5 Ketones by Oxypentafluorosulfanylation of Alkynes with SF5Cl and Oxygen
10.1021/acs.orglett.5c00884 · 2025 · External reference
Synthesis and Reaction of Pentafluorosulfanyl Chloride (SF5Cl)
10.1002/cjoc.70217 · 2025 · External reference
General Photo-Driven Chemoselective and Rapid Hydropentafluorosulfanylation of Alkenes via an Orchestrated Radical Chain Process
10.1021/jacs.5c14406 · 2025 · External reference
Substrate-Controlled Pentafluorosulfanylation of Activated Alkenes Containing the Benzimidazole Moiety with SF5Cl
10.1021/acs.joc.5c00103 · 2025 · External reference
Synthetic Access to Persulfuranyl Scaffolds via Direct and Indirect Methods
10.1021/acs.chemrev.5c00131 · 2025 · External reference
A General Leaving Group Assisted Strategy for Synthesis of Pentafluorosulfanyl Allylic Compounds
10.1126/sciadv.adw8408 · 2025 · External reference
Single-Step Photoinduced Radical Pentafluorosulfanylation and Cyclization of Alkenes for the Synthesis of SF5-Containing Cyclic Sulfinamides
10.1002/cjoc.70488 · 2026 · External reference
Understanding the Pentafluorosulfanyl Group and Property-Driven Design of SF5-Containing Compounds
10.1039/d5cs00566c · 2026 · External reference
Propellanes─From a Chemical Curiosity to “Explosive” Materials and Natural Products
10.1002/anie.201603951 · 2017 · External reference
Synthesis of BCP Benzylamines from 2-Azaallyl Anions and [1.1.1]Propellane
10.1002/anie.201810061 · 2018 · External reference
Recent Advances in the Applications of [1.1.1]Propellane in Organic Synthesis
10.1016/j.cclet.2020.04.023 · 2020 · External reference
Rationalizing the Diverse Reactivity of [1.1.1]Propellane through σ–π Delocalization
10.1039/d0sc01386b · 2020 · External reference
Dicarbofunctionalization of [1.1.1]Propellane Enabled by Nickel/Photoredox Dual Catalysis: One-Step Multicomponent Strategy for the Synthesis of BCP–Aryl Derivatives
10.1021/jacs.2c05304 · 2022 · External reference
Iodopentafluorosulfanylation of [1.1.1]Propellane and Further Functionalizations
10.1007/s11426-023-1715-2 · 2023 · External reference
Controlled Oligomerization of [1.1.1]Propellane through Radical Polarity Matching: Selective Synthesis of SF5- and CF3SF4-Containing [2]Staffanes
10.3762/bjoc.20.259 · 2024 · External reference
Tetrafluoro(aryl)sulfanylated Bicyclopentane Crystals that Self-Destruct upon Cooling
10.1021/jacs.4c08867 · 2025 · External reference
Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity
10.1021/jacs.6b13229 · 2017 · External reference
Strain Release – An Old Tool for New Transformations
10.1039/d0cc01771j · 2020 · External reference
One-Pot Synthesis of Strain-Release Reagents from Methyl Sulfones
10.1021/jacs.2c00923 · 2022 · External reference
Rapid and Scalable Halosulfonylation of Strain-Release Reagents
10.1002/anie.202213508 · 2023 · External reference
Strain-Release Photocatalysis
10.1021/jacs.3c08206 · 2023 · External reference
Visible Light-Induced Strain-Release Transformations of Bicyclo[1.1.0]butanes
10.1039/d4gc03193h · 2024 · External reference
Ring-Strain-Enabled Reaction Discovery: New Heterocycles from Bicyclo[1.1.0]butanes
10.1021/ar500437h · 2015 · External reference
Divergent Strain-Release Amino-Functionalization of [1.1.1]Propellane with Electrophilic Nitrogen-Radicals
10.1002/anie.202000140 · 2020 · External reference
Visible-Light-Induced 1,3-Aminopyridylation of [1.1.1]Propellane with N-Aminopyridinium Salts
10.1002/anie.202016156 · 2021 · External reference
Electrophilic Activation of [1.1.1]Propellane for the Synthesis of Nitrogen-Substituted Bicyclo[1.1.1]pentanes
10.1002/anie.202111291 · 2022 · External reference
Exploiting the sp2 Character of Bicyclo[1.1.1]pentyl Radicals in the Transition-Metal-Free Multicomponent Difunctionalization of [1.1.1]Propellane
10.1038/s41557-022-00979-0 · 2022 · External reference
A General and Modular Approach to BCP Alkylamines via Multicomponent Difunctionalization of [1.1.1]Propellane
10.1021/jacs.2c13298 · 2023 · External reference
Strain-Release Transformations of Bicyclo[1.1.0]butanes and [1.1.1]Propellanes
10.1016/j.tchem.2024.100070 · 2024 · External reference
Photocatalyzed Dual Strain Release of [1.1.1]Propellane with Diazo Compounds
10.1021/acscatal.4c00533 · 2024 · External reference
Recent Advances in Strain-Release Functionalization of [1.1.1]Propellanes Using Organometallic Reagents
10.1055/a-2669-6239 · 2026 · External reference
Electrophilic Activation of [1.1.1]Propellane by Silyl-Triflates
10.1021/acs.joc.5c03205 · 2026 · External reference
Bicyclobutanes: From Curiosities to Versatile Reagents and Covalent Warheads
10.1039/d2sc03948f · 2022 · External reference
Bicyclobutanes as Unusual Building Blocks for Complexity Generation in Organic Synthesis
10.1038/s42004-022-00811-3 · 2023 · External reference
Overcoming a Radical Polarity Mismatch in Strain-Release Pentafluorosulfanylation of [1.1.0]Bicyclobutanes: An Entryway to Sulfone- and Carbonyl-Containing SF5–Cyclobutanes
10.1002/anie.202319930 · 2024 · External reference
Strain-release trifluoromethoxylation and pentafluorosulfanoxylation of [1.1.0]bicyclobutanes: expanded access to fluorinated cyclobutene hybrid bioisosteres
10.1039/d4cc06616b · 2025 · External reference
Bench-stable Reagents for Modular Access to Persulfuranyl Scaffolds
10.1038/s41467-025-63621-w · 2025 · External reference
Recent Advances in the Strain-Release Driven Reactions of Bicyclobutanes: An Emerging Landscape in Organic Synthesis
10.1039/d6cs00010j · 2026 · External reference
Synthesis and Applications of Polysubstituted Bicyclo[1.1.0]butanes
10.1021/jacs.1c11244 · 2021 · External reference
State-of-the-Art Strategies for Lewis Acid-Catalyzed Strain-Release Cycloadditions of Bicyclo[1.1.0]butanes (BCBs)
10.1039/d4qo01741b · 2024 · External reference
Recent Advances in Photochemical Strain-Release Reactions of Bicyclo[1.1.0]butanes
10.1039/d4cc05108d · 2024 · External reference
Strain-Release-Driven 1,3-Halo-hydroxylamination of Bicyclo[1.1.0]butanes Enabled by Anomeric Amide Reagents
10.1021/acs.orglett.5c04047 · 2025 · External reference
Enantioselective Synthesis of 2-Substituted Bicyclo[1.1.1]pentanes via Sequential Asymmetric Imine Addition of Bicyclo[1.1.0]butanes and Skeletal Editing
10.1038/s41557-024-01710-x · 2025 · External reference
Strain-Release-Driven Synthesis of Pentafluorosulfanylated Four-Membered Rings under Energy Transfer Photocatalysis
10.1021/jacs.5c07138 · 2025 · External reference
Catalytic Asymmetric Strategies for Bicyclo[1.1.0]butane Transformations: Advances and Applications
10.31635/ccschem.025.202505825 · 2025 · External reference
Strain-Release Pentafluorosulfanylation of Carbonyl-Containing Disubstituted Bicyclobutanes: A Fortuitous Path to SF5-Containing Oxa[2.1.1]bicyclohexanes
10.1002/anie.4256865 · 2026 · External reference
The Renaissance of Strained 1-Azabicyclo[1.1.0]butanes as Useful Reagents for the Synthesis of Functionalized Azetidines
10.1039/d0ob01251c · 2020 · External reference
Divergent, Strain-Release Reactions of Azabicyclo[1.1.0]butyl Carbinols: Semipinacol or Spiroepoxy Azetidine Formation
10.1002/anie.202100583 · 2021 · External reference
Synthesis and Applications of Bicyclo[1.1.0]butyl and Azabicyclo[1.1.0]butyl Organometallics
10.1002/chem.202300008 · 2023 · External reference
Direct N–SF5 and N–SF4CF3 Bond Formation through Strain-Release Functionalization of 3-Substituted [1.1.0]Azabicyclobutanes
10.1021/jacs.5c07137 · 2025 · External reference
HFIP-Assisted Brønsted Acid-Catalyzed Ring Opening of 1-Azabicyclo[1.1.0]butane to Access Diverse C3-Quaternary Aza-Azetidines and Indole-Azetidines
10.1038/s41467-025-63680-z · 2025 · External reference
Divergent Synthesis of 1-Azabicyclo[n.1.1]alkane Bioisosteres via Photoinduced Palladium Catalysis
10.1021/jacs.5c09500 · 2025 · External reference
Modular Access to N–SF5 Azetidines
10.1021/jacs.5c10954 · 2025 · External reference
Aza-Darzens Type Reaction of Azirines: Access to Highly Substituted 1-Azabicyclo[1.1.0]butanes and Azetidines
10.1021/acs.joc.5c02748 · 2026 · External reference
Strain-Release Diversification of 1-Azabicyclobutanes via Bromide/Nickel Relay-Catalyzed 1,3-Bis-Carbofunctionalization
10.1002/anie.202522817 · 2026 · External reference
Catalytic Vicinal Difluorination of Olefins: Creating a Hybrid, Chiral Bioisostere of the Trifluoromethyl and Ethyl Groups
10.1021/acscatal.6b02155 · 2016 · External reference
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF3 and Et Using Matrix Metalloproteinases As Structural Probes
10.1021/acs.jmedchem.0c00648 · 2020 · External reference
Synthesis of meta-Substituted Arene Bioisosteres from [3.1.1]Propellane
10.1038/s41586-022-05290-z · 2022 · External reference
1-Azaspiro[3.3]heptane as a Bioisostere of Piperidine
10.1002/anie.202311583 · 2023 · External reference
Light-Driven Synthesis and Functionalization of Bicycloalkanes, Cubanes and Related Bioisosteres
10.1002/anie.202317333 · 2024 · External reference
Bicyclo[m.n.k]alkane Building Blocks as Promising Benzene and Cycloalkane Isosteres: Multigram Synthesis, Physicochemical and Structural Characterization
10.1002/chem.202303859 · 2024 · External reference
(Bio)isosteres of ortho- and meta-Substituted Benzenes
10.3762/bjoc.20.78 · 2024 · External reference
Isosteric 3D Bicyclo[1.1.1]Pentane (BCP) Core-Based Lipids for mRNA Delivery and CRISPR/Cas Gene Editing
10.1021/jacs.4c13154 · 2024 · External reference
Collective Synthesis of 1,2,4-Trisubstituted, meta- and ortho-Substituted Arene Bioisosteres from Bicyclobutanes
10.1038/s41557-026-02097-7 · 2026 · External reference
Liquid Crystals Based on Hypervalent Sulfur Fluorides: Pentafluorosulfuranyl as Polar Terminal Group
10.1002/(sici)1521-3773(19990712)38:13/14<1989::aid-anie1989>3.0.co;2-k · 1999 · External reference
Synthesis of Some Arylsulfur Pentafluoride Pesticides and Their Relative Activities Compared to the Trifluoromethyl Analogues
10.2533/000942904777678172 · 2004 · External reference
Synthetic Chemistry and Biological Activity of Pentafluorosulphanyl (SF5) Organic Molecules
10.1016/j.jfluchem.2012.06.030 · 2012 · External reference
Synthesis and Properties of Pentafluorosulfanyl Group (SF5)-Containing Meta-Diamide Insecticides
10.3390/molecules25235536 · 2020 · External reference
Antimalarial Drug Discovery: Progress and Approaches
10.1038/s41573-023-00772-9 · 2023 · External reference
The Pentafluorosulfanyl Group in Cannabinoid Receptor Ligands: Synthesis and Comparison with Trifluoromethyl and tert-Butyl Analogues
10.1039/c4ra01212g · 2014 · External reference
Evaluation of tert-Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities
10.1002/cmdc.201402502 · 2015 · External reference
Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement
10.1002/cmdc.201700356 · 2017 · External reference
CF3-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique tert-Butyl Group Analogue
10.1021/jacsau.4c00864 · 2024 · External reference
Application of the Bicyclo[1.1.1]pentane Motif as a Nonclassical Phenyl Ring Bioisostere in the Design of a Potent and Orally Active γ-Secretase Inhibitor
10.1021/jm300094u · 2012 · External reference
Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLA2 Inhibitor
10.1021/acsmedchemlett.6b00281 · 2017 · External reference
Saturated Bioisosteres of Benzene: Where to Go Next?
10.1039/c8ob02812e · 2019 · External reference
Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design
10.1021/acs.jmedchem.1c01215 · 2021 · External reference
Smallest Bicycles in Medicinal Chemistry: Where are we now?
10.1021/acs.chemrev.5c00779 · 2026 · External reference
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties
10.1021/acs.jmedchem.5b01654 · 2016 · External reference
Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1H-benzimidazol-2-ones as mGlu2 Receptor PAMs
10.1021/acsmedchemlett.9b00350 · 2020 · External reference
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
10.1021/jm901241e · 2009 · External reference
A Specific and Direct Comparison of the Trifluoromethyl and Pentafluorosulfanyl Groups on the Selective Dopamine D3 Antagonist 3-(3-{[4-Methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0]hexane Template
10.1016/j.bmcl.2010.06.018 · 2010 · External reference
Structure–Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97
10.1021/acsmedchemlett.5b00364 · 2015 · External reference
Design, Synthesis and Biological Evaluation of Novel Bicyclo[1.1.1]pentane-Based ω-Acidic Amino Acids as Glutamate Receptor Ligands
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Molecular Drug Targets and Structure Based Drug Design: A Holistic Approach
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Molecular Docking and Structure-Based Drug Design Strategies
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Generative Deep Learning for Targeted Compound Design
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TamGen: Drug Design with Target-Aware Molecule Generation through a Chemical Language Model
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Targeted Molecular Generation with Latent Reinforcement Learning
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Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?
10.1021/acs.jmedchem.5b01409 · 2016 · External reference
Synthesis of All-Carbon Disubstituted Bicyclo[1.1.1]pentanes by Iron-Catalyzed Kumada Cross-Coupling
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Chemoselective Csp2–H Radical Alkylation of Aryl Diazonium Salts with 1-Iodo-3-Pentafluorosulfanylbicyclo[1.1.1]pentane (SF5-BCP-I)
10.1002/cjoc.70007 · 2025 · External reference
Synthesis of Azo-Substituted Bicyclo[1.1.1]pentanes (BCPs) via Base-Promoted Halogen Atom Transfer
10.1021/acs.orglett.4c01546 · 2024 · External reference
Bicyclo[1.1.1]pentane-Derived Building Blocks for Click Chemistry
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Light-enabled scalable synthesis of bicyclo[1.1.1]pentane halides and their functionalizations
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Methylenespiro[2.3]hexanes via Nickel-Catalyzed Cyclopropanations with [1.1.1]Propellane
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Copper-Catalyzed Ring Opening of [1.1.1]Propellane with Alkynes: Synthesis of Exocyclic Allenic Cyclobutanes
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Isolation and Reactivity of Trifluoromethyl Iodonium Salts
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nBu4N+[AgI(CF3)2]−: Trifluoromethylated Argentate Derived from Fluoroform and Its Reaction with (Hetero)Aryl Diazonium Salts
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Copper-Catalyzed Trifluoromethylation of (Hetero)aryl Boronic Acid Pinacol Esters with YlideFluor
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Trifluoromethylation of Arenes and Heterocycles via a Bench-Stable Photocaged Trifluoromethylation Reagent
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(Hetero)aryl-SVI Fluorides: Synthetic Development and Opportunities
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Tecovirimat for the Treatment of Mpox
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Efficient Large-Scale Process for Tecovirimat via Reactive Distillation for the Preparation of Cycloheptatriene
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Electrochemically Enabled, Nickel-Catalyzed Amination
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Novel Inhibitors of the High-affinity L-Proline Transporter as Potential Therapeutic Agents for the Treatment of Cognitive Disorders
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