Frédéric Buron
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View article: Design, Synthesis and Evaluation of the First 2-Alkynyl(aza)indole 18F Probe Targeting α-Synuclein Aggregates
Design, Synthesis and Evaluation of the First 2-Alkynyl(aza)indole 18F Probe Targeting α-Synuclein Aggregates Open
Background/Objectives: The role of α-synuclein (α-syn) in the pathogenesis of Parkinson’s disease (PD) or neurodegenerative diseases such as Lewy body dementia (LBD) and multiple system atrophy (MSA) is commonly accepted. Through different…
View article: Synthesis and Reactivity of 1,4‐Ethano‐1,5‐Naphthyridine Derivatives Using Microwave Activation or Flow Chemistry
Synthesis and Reactivity of 1,4‐Ethano‐1,5‐Naphthyridine Derivatives Using Microwave Activation or Flow Chemistry Open
The design of some novel disubstituted 3,4‐dihydro‐2 H ‐1,4‐ethano‐1,5‐naphthyridine derivatives is reported under classical and flow methodologies. The series are developed from quinuclidinone, which afford versatile platforms bearing one…
View article: A continuous flow process for the Ireland–Claisen rearrangement
A continuous flow process for the Ireland–Claisen rearrangement Open
The transposition of an enantioselective Ireland–Claisen rearrangement was performed in a continuous flow reactor with a short residence time, achieving great stereocontrolled syntheses of vicinal stereogenic centers at room temperature.
View article: Synthesis, Luminescence and Relaxometric Properties of Macrocyclic Lanthanide Complexes Appended with an Imidazothiadiazole, a Heterocyclic Bioactive Scaffold
Synthesis, Luminescence and Relaxometric Properties of Macrocyclic Lanthanide Complexes Appended with an Imidazothiadiazole, a Heterocyclic Bioactive Scaffold Open
The syntheses of two macrocycles containing original imidazothiadiazole heterocycles are presented. The protonation constants of the ligands have been determined by potentiometry and photophysical measurements. The photophysical properties…
View article: Investigation of Ln<sup>3+</sup> complexation by a DOTA derivative substituted by an imidazothiadiazole: synthesis, solution structure, luminescence and relaxation properties
Investigation of Ln<sup>3+</sup> complexation by a DOTA derivative substituted by an imidazothiadiazole: synthesis, solution structure, luminescence and relaxation properties Open
A bioactive imidazothiadiazole heterocycle was appended to a macrocyclic ligand for direct Ln 3+ coordination as demonstrated by DFT and NMR. The resulting complexes are stable and inert and show interesting luminescent and relaxation feat…
View article: CCDC 2240715: Experimental Crystal Structure Determination
CCDC 2240715: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Innovative processes for natural active ingredients extraction and their online functionalization using flow chemistry
Innovative processes for natural active ingredients extraction and their online functionalization using flow chemistry Open
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View article: Stereoselective Synthesis of Iminosugar‐<i>C</i>‐Glycosides through Addition of Organometallic Reagents to <i>N</i>‐<i>tert</i>‐Butanesulfinyl Glycosylamines: A Comprehensive Study
Stereoselective Synthesis of Iminosugar‐<i>C</i>‐Glycosides through Addition of Organometallic Reagents to <i>N</i>‐<i>tert</i>‐Butanesulfinyl Glycosylamines: A Comprehensive Study Open
A comprehensive study of the preparation and reactivity of N‐tert ‐butanesulfinyl glycosylamines with simple Grignard and organo lithium reagents in batch vs . continuous flow chemistry is reported. As they readily react as latent imine eq…
View article: Access and Modulation of Substituted Pyrrolo[3,4-c]pyrazole-4,6-(2H,5H)-diones
Access and Modulation of Substituted Pyrrolo[3,4-c]pyrazole-4,6-(2H,5H)-diones Open
The first access to polyfunctionnalized pyrrolo[3,4-c]pyrazole-4,6-(2H,5H)-dione derivatives is reported. The series were generated from diethyl acetylenedicarboxylate and arylhydrazines, which afforded the key intermediates bearing two fu…
View article: CCDC 2276978: Experimental Crystal Structure Determination
CCDC 2276978: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Glycosaminoglycan Mimetics Obtained by Microwave-Assisted Sulfation of Marine Bacterium Sourced Infernan Exopolysaccharide
Glycosaminoglycan Mimetics Obtained by Microwave-Assisted Sulfation of Marine Bacterium Sourced Infernan Exopolysaccharide Open
Sulfated glycosaminoglycans (GAGs) are fundamental constituents of both the cell surface and extracellular matrix. By playing a key role in cell-cell and cell-matrix interactions, GAGs are involved in many physiological and pathological pr…
View article: CCDC 2104956: Experimental Crystal Structure Determination
CCDC 2104956: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: A Facile One-Pot Synthesis of New Poly Functionalized Pyrrolotriazoles via a Regioselective Multicomponent Cyclisation and Suzuki–Miyaura Coupling Reactions
A Facile One-Pot Synthesis of New Poly Functionalized Pyrrolotriazoles via a Regioselective Multicomponent Cyclisation and Suzuki–Miyaura Coupling Reactions Open
The first access to N-1, N-4 disubstituted pyrrolo[2,3-d][1,2,3]triazoles is reported. The series were generated using a “one-pot” MCR, leading to a single regioisomer of the attempted heteroaromatic skeleton in good yields. Next, the func…
View article: Selection of Bis-Indolyl Pyridines and Triphenylamines as New Inhibitors of SARS-CoV-2 Cellular Entry by Modulating the Spike Protein/ACE2 Interfaces
Selection of Bis-Indolyl Pyridines and Triphenylamines as New Inhibitors of SARS-CoV-2 Cellular Entry by Modulating the Spike Protein/ACE2 Interfaces Open
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the infectious agent that has caused the current coronavirus disease (COVID) pandemic. Viral infection relies on the viral S (spike) protein/cellular receptor ACE2 interaction.
View article: Design and biological evaluation of substituted 5,7-dihydro-6 <i>H</i> -indolo[2,3- <i>c</i> ]quinolin-6-one as novel selective Haspin inhibitors
Design and biological evaluation of substituted 5,7-dihydro-6 <i>H</i> -indolo[2,3- <i>c</i> ]quinolin-6-one as novel selective Haspin inhibitors Open
A library of substituted indolo[2,3-c]quinolone-6-ones was developed as simplified Lamellarin isosters. Synthesis was achieved from indole after a four-step pathway sequence involving iodination, a Suzuki-Miyaura cross-coupling reaction, a…
View article: Modeling Temperature and Species Concentration Profiles on a Continuous-Flow Reactor Applied to Aldol Condensation
Modeling Temperature and Species Concentration Profiles on a Continuous-Flow Reactor Applied to Aldol Condensation Open
This paper presents the modeling of a continuous-flow reactor used for the synthesis of organic products. The finite element method software, COMSOL Multiphysics, was used to model transport phenomena and reaction kinetics. The temperature…
View article: Synthesis of novel series of 3,5-disubstituted imidazo[1,2-<i>d</i>] [1,2,4]thiadiazoles involving S<sub>N</sub>Ar and Suzuki–Miyaura cross-coupling reactions
Synthesis of novel series of 3,5-disubstituted imidazo[1,2-<i>d</i>] [1,2,4]thiadiazoles involving S<sub>N</sub>Ar and Suzuki–Miyaura cross-coupling reactions Open
A convenient design of 3,5-disubstituted imidazo[1,2- d ][1,2,4]thiadiazoles is reported from 2-mercaptoimidazole, which afforded a versatile platform that was then used to access a variety of original heterocycles.
View article: Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-d]Pyrimidine Series as Novel PI3K/mTOR Inhibitors
Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-d]Pyrimidine Series as Novel PI3K/mTOR Inhibitors Open
This work describes the synthesis, enzymatic activities on PI3K and mTOR, in silico docking and cellular activities of various uncommon 2,4,7 trisubstituted pyrido[3,2-d]pyrimidines. The series synthesized offers a chemical diversity in C-…
View article: Design, Synthesis, In Silico and In Vitro Studies for New Nitric Oxide-Releasing Indomethacin Derivatives with 1,3,4-Oxadiazole-2-thiol Scaffold
Design, Synthesis, In Silico and In Vitro Studies for New Nitric Oxide-Releasing Indomethacin Derivatives with 1,3,4-Oxadiazole-2-thiol Scaffold Open
Starting from indomethacin (IND), one of the most prescribed non-steroidal anti-inflammatory drugs (NSAIDs), new nitric oxide-releasing indomethacin derivatives with 1,3,4-oxadiazole-2-thiol scaffold (NO-IND-OXDs, 8a–p) have been developed…
View article: Development of PET Radioligands Targeting COX-2 for Colorectal Cancer Staging, a Review of in vitro and Preclinical Imaging Studies
Development of PET Radioligands Targeting COX-2 for Colorectal Cancer Staging, a Review of in vitro and Preclinical Imaging Studies Open
Colorectal cancer (CRC) is the second most common cause of cancer death, making early diagnosis a major public health challenge. The role of inflammation in tumorigenesis has been extensively explored, and among the identified markers of i…
View article: Aminations and arylations by direct C–O activation for the design of 7,8-dihydro-6<i>H</i>-5,8-ethanopyrido[3,2-<i>d</i>]pyrimidines
Aminations and arylations by direct C–O activation for the design of 7,8-dihydro-6<i>H</i>-5,8-ethanopyrido[3,2-<i>d</i>]pyrimidines Open
A convenient design of 7,8-dihydro-6H-5,8-ethanopyrido[3,2-d]pyrimidines is reported from quinuclidinone, which afforded versatile platforms that were then used to access a variety of original heterocycles.
View article: Prodromal neuroinflammatory, cholinergic and metabolite dysfunction detected by PET and MRS in the TgF344-AD transgenic rat model of AD: a collaborative multi-modal study
Prodromal neuroinflammatory, cholinergic and metabolite dysfunction detected by PET and MRS in the TgF344-AD transgenic rat model of AD: a collaborative multi-modal study Open
Mouse models of Alzheimer's disease (AD) are valuable but do not fully recapitulate human AD pathology, such as spontaneous Tau fibril accumulation and neuronal loss, necessitating the development of new AD models. The transgenic (TG) TgF3…
View article: Neuroprotective and anti-inflammatory effects of a therapy combining agonists of nicotinic α7 and σ1 receptors in a rat model of Parkinson's disease
Neuroprotective and anti-inflammatory effects of a therapy combining agonists of nicotinic α7 and σ1 receptors in a rat model of Parkinson's disease Open
To date there is no treatment able to stop or slow down the loss of dopaminergic neurons that characterizes Parkinson's disease. It was recently observed in a rodent model of Alzheimer's disease that the interaction between the a7 subtype …
View article: New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile
New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile Open
Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an …