(3-Chlorophenyl){2-ethoxy-5-[(Z)-hydroxy(phenyl)methylidene]cyclopenta-1,3-dien-1-yl}methanone

Autor: Mihaela-Liliana Tinţaş, Richard A. Varga, Ion Grosu, Elena Bogdan

Publikováno v: Acta Crystallographica Section E, Vol 68, Iss 2, Pp o310-o311 (2012)

The title compound, C21H17ClO3, which crystallizes as one of two possible oxo/hydroxy-fulvene prototropic tautomers, possesses a strong intramolecular O—H...O hydrogen bond that closes a seven-membered ring. The dihedral angles between the central

Externí odkaz: https://doaj.org/article/6efb162110a64a4694a3182221bd9bea

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

Access to Highly Enantioenriched Donepezil-like 1,4-Dihydropyridines as Promising Anti-Alzheimer Prodrug Candidates via Enantioselective Tsuji Allylation and Organocatalytic Aza-Ene-Type Domino Reactions

Autor: Vincent Levacher, Rabah Azzouz, Emilie Petit, Ludovic Peauger, Vincent Gembus, Mihaela-Liliana Ţînţaş, Cyril Papamicaël, Laetitia Bailly

Publikováno v: Journal of Organic Chemistry
Journal of Organic Chemistry, American Chemical Society, 2018, 83 (17), pp.10231-10240. ⟨10.1021/acs.joc.8b01442⟩

International audience; This work aims at exploiting both the enantioselective Tsuji allylation of allyl carbonate 6 and an organocatalytic aza-ene-type domino reaction between enal 3a and β-enaminone 4a to develop a straightforward access to all of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c32915afd6ef1875d663e0f8f7c2f9b
https://pubmed.ncbi.nlm.nih.gov/30004228

Dihydroquinoline Carbamate Derivatives as 'Bio-oxidizable' Prodrugs for Brain Delivery of Acetylcholinesterase Inhibitors: [11C] Radiosynthesis and Biological Evaluation

Autor: Mihaela-Liliana Ţînţaş, Cyril Papamicaël, Vincent Levacher, Vincent Gembus, Florent Alix, Fabienne Gourand, Martine Dhilly, Francis Marsais, Pierre Bohn, Meziane Ibazizene, Louisa Barré

Publikováno v: ACS Chemical Neuroscience. 6:737-744

With the aim of improving the efficiency of marketed acetylcholinesterase (AChE) inhibitors in the symptomatic treatment of Alzheimer's disease, plagued by adverse effects arising from peripheral cholinergic activation, this work reports a biological

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::09dcfcef1c2bc249280efdcfb9ea021f
https://doi.org/10.1021/cn5003539

Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a 'Bio-Oxidizable' Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation

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

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2017, 60 (13), pp.5909-5926. ⟨10.1021/acs.jmedchem.7b00702⟩

International audience; With the aim of reducing side effects of acetylcholinesterase inhibitors (AChEIs) during symptomatic treatment of Alzheimer’s disease, we report herein a new class of donepezil-based “bio-oxidizable” prodrugs 1 designed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33f7863134daf7472be7d0ef7dc634b0
https://hal.archives-ouvertes.fr/hal-02043729