Search Results - "Crestey, François"
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Design, Synthesis, and Biological Evaluation of Erythrina Alkaloid Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists
Published in Journal of medicinal chemistry (12-12-2013)“…The synthesis of a new series of Erythrina alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR)…”
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2
Expedite Protocol for Construction of Chiral Regioselectively N-Protected Monosubstituted Piperazine, 1,4-Diazepane, and 1,4-Diazocane Building Blocks
Published in Journal of organic chemistry (07-08-2009)“…This paper describes the first study of solution-phase synthesis of chiral monosubstituted piperazine building blocks from nosylamide-activated aziridines. The…”
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3
Total synthesis of ascididemin via anionic cascade ring closure
Published in Chemical communications (Cambridge, England) (18-09-2012)“…A new and convergent synthesis of ascididemin is presented. Using an anionic cascade ring closure as the key step, this natural product is obtained in 45%…”
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4
Chemo- and Regioselective Functionalization of Nortrilobolide: Application for Semisynthesis of the Natural Product 2‑Acetoxytrilobolide
Published in Journal of natural products (Washington, D.C.) (26-06-2015)“…The difference in reactivity of the hexaoxygenated natural product thapsigargin (1) and the pentaoxygenated nortrilobolide (3) was compared in order to develop…”
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5
Concise synthesis of thapsigargin from nortrilobolide
Published in Tetrahedron letters (21-10-2015)“…[Display omitted] Herein, we describe an expedient synthesis of the hexaoxygenated guaianolide thapsigargin (1), a potent inhibitor of the sarco/endoplasmic…”
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A strategic approach to [6,6]-bicyclic lactones: application towards the CD fragment of DHβE
Published in Beilstein journal of organic chemistry (22-05-2017)“…We report an effective synthetic protocol to access [6,6]-bicyclic lactone moieties through a regio- and stereoselective intramolecular Mizoroki-Heck…”
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7
Trifunctionalization of the Purine Scaffold Using Mg and Zn Organometallic Intermediates
Published in Organic letters (18-02-2011)“…Starting from an appropriate 6-chloro-2-TMS-purine derivative, a regioselective functionalization of the purine scaffold was achieved successively at positions…”
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Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts
Published in Journal of medicinal chemistry (22-02-2018)“…We describe the synthesis of tetrahydroisoquinolines and tetrahydroisoquinolinium salts together with their pharmacological properties at various nicotinic…”
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9
Concise synthesis of new bridged-nicotine analogues
Published in Tetrahedron (04-02-2012)“…This study describes a very efficient strategy for the synthesis of two new bridged-nicotine analogues. Starting from either 4- or 3-chloropyridine the desired…”
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10
Microwave-Assisted Ring-Opening of Activated Aziridines with Resin-Bound Amines
Published in Journal of organic chemistry (02-05-2008)“…This paper describes the first study of nucleophilic ring-opening of nosylamide-activated aziridines under microwave irradiation conditions in solid-phase…”
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11
Radiosynthesis and preclinical evaluation of [11C]Cimbi‐701 – Towards the imaging of cerebral 5‐HT7 receptors
Published in Journal of labelled compounds & radiopharmaceuticals (01-02-2020)“…The serotonin 7 (5‐HT7) receptor is suggested to be involved in a broad variety of CNS disorders, but very few in vivo tools exist to study this important…”
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12
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors
Published in ACS medicinal chemistry letters (09-04-2015)“…Conformational restriction of the pyrrolidine nitrogen in nicotine by the introduction of an ethylene bridge provided a potent and selective antagonist of the…”
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13
Efficient loading of primary alcohols onto a solid phase using a trityl bromide linker
Published in Tetrahedron letters (06-10-2008)“…The Letter describes an improved, rapid and mild strategy for the loading of primary alcohols onto a polystyrene trityl resin via a highly reactive trityl…”
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14
Identification and Electrophysiological Evaluation of 2‑Methylbenzamide Derivatives as Nav1.1 Modulators
Published in ACS chemical neuroscience (19-08-2015)“…Voltage-gated sodium channels (Nav) are crucial to the initiation and propagation of action potentials (APs) in electrically excitable cells, and during the…”
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15
A new and efficient synthesis of 2-azatryptophans
Published in Tetrahedron (14-08-2006)“…This paper describes a new and simple synthesis of 2-azatryptophans in five steps from 2-ethylaniline. This methodology allows to obtain either the amino acid…”
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16
Design and synthesis of a new indazole library: direct conversion of N-methoxy- N-methylamides (Weinreb amides) to 3-keto and 3-formylindazoles
Published in Tetrahedron (08-01-2007)“…Nucleophilic addition of Grignard or lithiated reagents on the new Weinreb amides 3 and 4 afforded efficiently the corresponding ketones and allowed the design…”
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17
New practical access to 2-azatryptophans and dehydro derivatives via the Wittig–Horner reaction
Published in Tetrahedron letters (02-04-2007)“…The Wittig–Horner reaction of protected 3-formylindazoles 1 with (±)- N-(benzyloxycarbonyl)-α-phosphonoglycine trimethyl ester 2 has been developed as a new…”
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A small molecule activator of Nav1.1 channels increases fast‐spiking interneuron excitability and GABAergic transmission in vitro and has anti‐convulsive effects in vivo
Published in The European journal of neuroscience (01-08-2017)“…Nav1.1 (SCN1A) channels primarily located in gamma‐aminobutyric acid (GABA)ergic fast‐spiking interneurons are pivotal for action potential generation and…”
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19
Direct Cu-mediated aromatic 18 F-labeling of highly reactive tetrazines for pretargeted bioorthogonal PET imaging
Published in Chemical science (Cambridge) (15-09-2021)“…Pretargeted imaging can be used to visualize and quantify slow-accumulating targeting vectors with short-lived radionuclides such as fluorine-18 - the most…”
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20
Direct Cu-mediated aromatic 18F-labeling of highly reactive tetrazines for pretargeted bioorthogonal PET imaging
Published in Chemical science (Cambridge) (15-09-2021)“…Pretargeted imaging can be used to visualize and quantify slow-accumulating targeting vectors with short-lived radionuclides such as fluorine-18 – the most…”
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