Zobrazeno 1 - 10 of 42 pro vyhledávání: '"Marc, Since"'
1
Akademický článek
Synthesis of Nitrostyrylthiazolidine-2,4-dione Derivatives Displaying Antileishmanial Potential
Autor: Omar Khoumeri, Sébastien Hutter, Nicolas Primas, Caroline Castera-Ducros, Sandra Carvalho, Susan Wyllie, Mohamed Lotfi Efrit, Dimitri Fayolle, Marc Since, Patrice Vanelle, Pierre Verhaeghe, Nadine Azas, Hussein El-Kashef
Publikováno v: Pharmaceuticals, Vol 17, Iss 7, p 878 (2024)
A series of 61 thiazolidine-2,4-diones bearing a styryl group at position 5 was synthesized in 2–5 steps and their structure was proved by elemental and spectral analyses. The compounds obtained were evaluated in vitro against the promastigote stag
Externí odkaz: https://doaj.org/article/19bbdde0254342f6abec98d71ef49a9d
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2
Akademický článek
A Biomimetic Multiparametric Assay to Characterise Anti-Amyloid Drugs
Autor: Willy Smeralda, Marc Since, Sophie Corvaisier, Dimitri Fayolle, Julien Cardin, Sylvain Duprey, Jean-Pierre Jourdan, Christophe Cullin, Aurélie Malzert-Freon
Publikováno v: International Journal of Molecular Sciences, Vol 24, Iss 23, p 16982 (2023)
Alzheimer’s disease (AD) is the most widespread form of senile dementia worldwide and represents a leading socioeconomic problem in healthcare. Although it is widely debated, the aggregation of the amyloid β peptide (Aβ) is linked to the onset an
Externí odkaz: https://doaj.org/article/e81db4bb423e4ec9acdf87194b3ea894
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3
Akademický článek
Improving Aqueous Solubility and In Vitro Pharmacokinetic Properties of the 3-Nitroimidazo[1,2-a]pyridine Antileishmanial Pharmacophore
Autor: Romain Paoli-Lombardo, Nicolas Primas, Sandra Bourgeade-Delmas, Sébastien Hutter, Alix Sournia-Saquet, Clotilde Boudot, Emilie Brenot, Caroline Castera-Ducros, Sophie Corvaisier, Marc Since, Aurélie Malzert-Fréon, Bertrand Courtioux, Alexis Valentin, Pierre Verhaeghe, Nadine Azas, Pascal Rathelot, Patrice Vanelle
Publikováno v: Pharmaceuticals, Vol 15, Iss 8, p 998 (2022)
An antileishmanial structure–activity relationship (SAR) study focused on positions 2 and 8 of the imidazo[1,2-a]pyridine ring was conducted through the synthesis of 22 new derivatives. After being screened on the promatigote and axenic amastigote
Externí odkaz: https://doaj.org/article/83013cdfb1b946f190f6b3a926203f86
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4
Star-like poly(peptoid)s with selective antibacterial activity
Autor: Pedro Salas-Ambrosio, Antoine Tronnet, Mostafa Badreldin, Luzangel Reyes, Marc Since, Sandra Bourgeade-Delmas, Bruno Dupuy, Pierre Verhaeghe, Colin Bonduelle
Publikováno v: Polymer Chemistry
Polymer Chemistry, 2022, 13 (5), pp.600-612. ⟨10.1039/D1PY01529J⟩
International audience; We developed new macromolecular engineering approaches enabling the preparation of star-like polypeptoids by ring-opening polymerization. Parallely to the evaluation of their cytotoxicity of the HepG2 human cell line, their sc
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4318ea43d34e094ec22ad35e3de1489e
https://doi.org/10.1039/d1py01529j
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5
Akademický článek
Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment
Autor: Thomas Adnet, Anne-Claire Groo, Céline Picard, Audrey Davis, Sophie Corvaisier, Marc Since, Frédéric Bounoure, Christophe Rochais, Loïc Le Pluart, Patrick Dallemagne, Aurélie Malzert-Fréon
Publikováno v: Pharmaceutics, Vol 12, Iss 3, p 251 (2020)
Direct nose-to-brain delivery has been raised as a non-invasive powerful strategy to deliver drugs to the brain bypassing the blood-brain barrier (BBB). This study aimed at preparing and characterizing an innovative composite formulation, associating
Externí odkaz: https://doaj.org/article/fbb8e2487303402abfb8886053e0b2c5
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6
Synthesis of antiplasmodial 2-aminothieno[3,2-d]pyrimidin-4(3H)-one analogues using the scaffold hopping strategy
Autor: Romain Mustière, Prisca Lagardère, Sébastien Hutter, Viviana Dell’Orco, Nadia Amanzougaghene, Shahin Tajeri, Jean-François Franetich, Sophie Corvaisier, Marc Since, Aurélie Malzert-Fréon, Nicolas Masurier, Vincent Lisowski, Pierre Verhaeghe, Dominique Mazier, Nadine Azas, Patrice Vanelle, Nicolas Primas
Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2022, 241, pp.114619. ⟨10.1016/j.ejmech.2022.114619⟩
International audience; Gamhepathiopine (also known as M1), is a multi-stage acting antiplasmodial 2-tert-butylaminothieno[3,2-d]pyrimidin-4(3H)-one hydrochloride that was first described in 2015. The development of this compound is limited by poor m
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84bfd963e0e1116d6ce6680442b337fa
https://hal.science/hal-03737417
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7
Cyclic Poly(α-peptoid)s by Lithium bis(trimethylsilyl)amide (LiHMDS)-Mediated Ring-Expansion Polymerization: Simple Access to Bioactive Backbones
Autor: Pierre Verhaeghe, Sébastien Lecommandoux, Antoine Tronnet, Marc Since, Jean-Luc Stigliani, Pedro Salas-Ambrosio, Sandra Bourgeade-Delmas, Bruno Dupuy, Amelie Vax, Colin Bonduelle
Publikováno v: Journal of the American Chemical Society
Journal of the American Chemical Society, American Chemical Society, 2021, 143 (10), pp.3697-3702. ⟨10.1021/jacs.0c13231⟩
International audience; Cyclic polymers display unique physicochemical and biological properties. However, their development is often limited by their challenging preparation. In this work, we present a simple route to cyclic poly(α-peptoids) from N
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8dcc10241c6e3ed52645b286da5d91f
https://doi.org/10.1021/jacs.0c13231
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8
Akademický článek
Inhibiting Acetylcholinesterase to Activate Pleiotropic Prodrugs with Therapeutic Interest in Alzheimer’s Disease
Autor: François-Xavier Toublet, Cédric Lecoutey, Julien Lalut, Bérénice Hatat, Audrey Davis, Marc Since, Sophie Corvaisier, Thomas Freret, Jana Sopkova de Oliveira Santos, Sylvie Claeysen, Michel Boulouard, Patrick Dallemagne, Christophe Rochais
Publikováno v: Molecules, Vol 24, Iss 15, p 2786 (2019)
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disease which is still poorly understood. The drugs currently used against AD, mainly acetylcholinesterase inhibitors (AChEI), are considered clinically insufficient and are responsible
Externí odkaz: https://doaj.org/article/8a4bfc5092844dbebc8144c2bdd2f874
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10
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT6 receptor antagonist with therapeutic interest in Alzheimer’s disease
Autor: Thomas Freret, Michel Boulouard, Audrey Davis, Marc Since, Bérénice Hatat, Sylvie Claeysen, François-Xavier Toublet, Patrick Dallemagne, Julien Lalut, Jana Sopkova-de Oliveira Santos, Sophie Corvaisier, Christophe Rochais, Cédric Lecoutey
Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2021, 210, pp.113059. ⟨10.1016/j.ejmech.2020.113059⟩
European Journal of Medicinal Chemistry, 2021, 210, pp.113059. ⟨10.1016/j.ejmech.2020.113059⟩
International audience; Beside acetylcholinesterase, butyrylcholinesterase could be considered as a putative target of interest for the symptomatic treatment of Alzheimer's disease (AD). As a result of complexity of AD, no molecule has been approved
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2aa2b8af7388914a57c9b97ea2cbffa1
https://hal.archives-ouvertes.fr/hal-03082877
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