Sylvain Rault

Centre d'Etudes et de Recherche sur le Médicament de Normandie

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i-10 index

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Document Type

Co-Authors

Jean‐Charles Lancelot

Centre d'Etudes et de Recherche sur le Médicament de Normandie

103

Patrick Dallemagne

Université de Caen Normandie

Jana Sopková−de Oliveira Santos

Université de Caen Normandie

M. ROBBA

Galen University

Ronan Bureau

Normandie Université

Valérie Collot

Normandie Université

Anne Sophie Voisin‐Chiret

Université de Caen Normandie

Frédéric Fabis

Université de Caen Normandie

Alexandre Bouillon

Laboratoires Gilbert (France)

Aurélien Lesnard

Université de Caen Normandie

Cooperative Institutions

Centre National de la Recherche Scientifique

282

Université de Caen Normandie

216

Normandie Université

142

Inserm

141

Centre d'Etudes et de Recherche sur le Médicament de Normandie

125

Université Paris Cité

Laboratoire de Chimie

Sorbonne Université

Aix-Marseille Université

Université de Rouen Normandie

Author Statistics

Papers

Citation

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Research Field

A Convenient Synthesis of Dihydro‐ and Tetrahydro‐1,3‐thiazine Derivatives from β‐Aryl‐β‐amino Acids.

ChemInform (2004)

Nicolas Leflemme Patrick Dallemagne Sylvain Rault

Abstract For Abstract see ChemInform Abstract in Full Text.

Thiazine

10.1002/chin.200421146

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Citations (0)

ChemInform Abstract: A Rapid and Versatile Synthesis of Novel Pyrimido[5,4‐b]carbazoles.

ChemInform (2010)

Anna Caruso Jean‐Charles Lancelot Hussein El‐Kashef Maria Stefania Sinicropi Rémi Legay

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

10.1002/chin.201014159

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Citations (0)

Synthesis and Study of the Stability of 3b,4,4a,5-Tetrahydrothieno[2',3':5,4]cyclopenta[2,3-b]aziridine Derivatives

Heterocycles (1987)

M. ROBBA Patrick Dallemagne Sylvain Rault Daniel Maume

tetrahydrothiem[?',3' :5,4]cyclopenta [2,3-b]

Aziridine

10.3987/r-1987-06-1449

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Citations (9)

New Benzo[h][1,6]naphthyridine and Azepino[3,2-c]quinoline Derivatives as Selective Antagonists of 5-HT₄ Receptors: Binding Profile and Pharmacological Characterization

Journal of Medicinal Chemistry (2002)

Antoine Hinschberger Sabrina Butt Véronique Lelong Michel Boulouard Aline Dumuis

A series of benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives were prepared and evaluated to determine the necessary requirements for high affinity on the 5-HT(4) receptors and high selectivity versus other receptors. The compounds were synthesized by substituting the chlorine atom of benzonaphthyridines and azepinoquinolines with various N-alkyl-4-piperidinylmethanolates. They were evaluated in binding assays with [(3)H]GR 113808 as the 5-HT(4) receptor radioligand. The affinity values (K(i) or inhibition percentages) depended upon the substituent on the aromatic ring on one hand and the substituent on the lateral piperidine chain on the other hand. A chlorine atom produced a marked drop in activity while a N-propyl or N-butyl group gave compounds with nanomolar affinities (1 < K(i) < 10 nM). Among the most potent ligands (3a, 4a, 5a), 4a was selected on the basis of its high affinity and selectivity for pharmacological screening and was evaluated in vivo in specific tests. This compound reveals itself as an antagonist/low partial agonist in the COS-7 cells stably expressing the 5-HT(4(a)) receptor. Derivative 4a also showed in vivo potent analgesic activity in the writhing test at very low doses.

Quinoline

10.1021/jm020954v

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Citations (48)

Novel Oxybispyridylboronic Acids: Synthesis and Study of Their Reactivity in Suzuki‐Type Cross‐Coupling Reactions.

ChemInform (2007)

Anne Sophie Voisin Alexandre Bouillon Inmaculada Berenguer Jean‐Charles Lancelot Aurélien Lesnard

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Reactivity

Coupling reaction

10.1002/chin.200712181

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Citations (0)

Protected Indazole Boronic Acid Pinacolyl Esters: Facile Syntheses and Studies of Reactivities in Suzuki-Miyaura Cross-Coupling and Hydroxydeboronation Reactions

Synlett (2009)

Valérie Collot François Crestey Elodie Lohou Silvia Stiebing Sylvain Rault

The paper describes a rapid and efficient synthesis for the isolation of protected indazolylboronic esters. These compounds were synthesized by reaction between prepared protected haloindazoles and bis(pinacolato)diboron. The effects of solvent, temperature, reaction time, and the nature of halogen atom as well as protecting group were investigated. Additionaly, these compounds reacted either with aryl halides in a Suzuki-Miyaura cross-coupling reaction or with hydrogen peroxide in a hydroxydeboronation reaction showing the potential access to new aryl and hydroxyindazole libraries.

Indazole

Boronic acid

Coupling reaction

Aryl halide

10.1055/s-0028-1087922

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Citations (10)

Sonogashira cross-coupling reaction of 3-iodoindazoles with various terminal alkynes: a mild and flexible strategy to design 2-aza tryptamines

Tetrahedron Letters (2002)

Diana-Aurora Arnăutu Valérie Collot Javier Calvo Ros C. Alayrac B. Witulski

Sonogashira coupling

Tryptamines