Straightforward Access to a New Class of Dual DYRK1A/CLK1 Inhibitors Possessing a Simple Dihydroquinoline Core

Autor: Mihaela-Liliana Ţînţaş, Ludovic Peauger, Florent Alix, Cyril Papamicaël, Thierry Besson, Jana Sopková-de Oliveira Santos, Vincent Gembus, Vincent Levacher

Publikováno v: Molecules, Vol 28, Iss 1, p 36 (2022)

The DYRK (Dual-specificity tyrosine phosphorylation-regulated kinase) family of protein kinases is involved in the pathogenesis of several neurodegenerative diseases. Among them, the DYRK1A protein kinase is thought to be implicated in Alzheimer’s

Externí odkaz: https://doaj.org/article/7fdc388c63c14f89a04942f33f00368b

Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy

Autor: Anaïs Barré, Rabah Azzouz, Vincent Gembus, Cyril Papamicaël, Vincent Levacher

Publikováno v: Molecules, Vol 24, Iss 7, p 1264 (2019)

Despite their side effects, cholinesterase (ChE) inhibitors remain the only approved drugs to treat Alzheimer’s disease patients, along with the N-methyl-d-aspartate (NMDA) receptor antagonist memantine. In the last few years, the dual-specificity

Externí odkaz: https://doaj.org/article/c64dc07cfc994ea19478c352260713e9

Novel donepezil-like N -benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine 'bio-oxidizable' prodrugs: Synthesis, biological evaluation and structure-activity relationship

Autor: Jana Sopkova-de Oliveira Santos, Cyril Papamicaël, Rabah Azzouz, Vincent Gembus, Ludovic Peauger, Mihaela-Liliana Ţînţaş, Vincent Levacher

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2018, 145, pp.165-190. ⟨10.1016/j.ejmech.2017.12.084⟩

International audience; As an extension of our previous work on donepezil-based “bio-oxidizable” prodrug approach, two new classes of N-benzylpyridinium donepezil analogues in tetralone B2 and acetophenone B3 series and a new set of indanone deri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d8b24b02728ee050843218b9f6525ad
https://doi.org/10.1016/j.ejmech.2017.12.084

An Overview of the Synthesis of Highly Versatile N-Hydroxysuccinimide Esters

Autor: Vincent Levacher, Cyril Papamicaël, Vincent Gembus, Mihaela-Liliana Ţînţaş, Anaïs Barré

Publikováno v: SYNTHESIS
SYNTHESIS, Georg Thieme Verlag, 2017, 49 (3), pp.472-483. ⟨10.1055/s-0036-1588607⟩

N-Hydroxysuccinimide esters (NHS-esters) are important and widely used tools in various areas of chemistry including peptide synthesis, bioconjugate chemistry, functionalized materials and polymers. The usual strategy employed to prepare these active

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f1e238a03636cc19adefcea8ef21caf
https://doi.org/10.1055/s-0036-1588607

Dihydroquinoline Carbamate DQS1-02 as a Prodrug of a Potent Acetylcholinesterase Inhibitor for Alzheimer’s Disease Therapy: Multigram-Scale Synthesis, Mechanism Investigations, in Vitro Safety Pharmacology, and Preliminary in Vivo Toxicology Profile

Autor: Philippe Chan, Muriel Sebban, Florent Alix, Gaël Coadou, Lina Truong, Vincent Levacher, Hassan Oulyadi, Marie Hubert-Roux, Cyril Papamicaël, Vincent Gembus, Laurent Coquet

Publikováno v: ACS Omega
ACS Omega, ACS Publications, 2018, 3 (12), pp.18387-18397. ⟨10.1021/acsomega.8b02121⟩
ACS Omega, Vol 3, Iss 12, Pp 18387-18397 (2018)
ACS Omega, 2018, 3 (12), pp.18387-18397. ⟨10.1021/acsomega.8b02121⟩

International audience; We previously characterized a set of potent pseudo-irreversible inhibitors of acetylcholinesterase (AChE) based on a redox prodrug strategy. Among the various synthesized prodrugs, compound 1, namely DQS1-02, displayed favorab

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::847d90956bb3ba058ef61b4cc32e7148
https://hal.archives-ouvertes.fr/hal-03134333