Medicinal Chemistry Based Approaches and Nanotechnology-Based Systems to Improve CNS Drug Targeting and Delivery

Autor: Michel Khrestchatisky, Patrick Vlieghe

Publikováno v: Medicinal Research Reviews. 33:457-516

The central nervous system (CNS) is protected by various barriers, which regulate nervous tissue homeostasis and control the selective and specific uptake, efflux, and metabolism of endogenous and exogenous molecules. Among these barriers is the bloo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::024b6173806b33fc22c0c74fef75c46d
https://doi.org/10.1002/med.21252

Synthetic therapeutic peptides: science and market

Autor: Patrick Vlieghe, Michel Khrestchatisky, Jean Martinez, Vincent Lisowski

Publikováno v: Drug Discovery Today. 15:40-56

The decreasing number of approved drugs produced by the pharmaceutical industry, which has been accompanied by increasing expenses for R&D, demands alternative approaches to increase pharmaceutical R&D productivity. This situation has contributed to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0d52de5e595b525cc8e372c2addd3b5
https://doi.org/10.1016/j.drudis.2009.10.009

New Bicyclam−AZT Conjugates: Design, Synthesis, Anti-HIV Evaluation, and Their Interaction with CXCR-4 Coreceptor

Autor: Patrick Vlieghe, Jean-Louis Kraus, Jean Dessolin, Jean-Claude Chermann, Pascale Galea

Publikováno v: Journal of Medicinal Chemistry. 42:229-241

We report the synthesis of mono- and bis-tetraazamacrocycle-AZT conjugates. All new compounds were screened for their ability to inhibit HIV-1 replication in MT4 cell line and were compared to AZT alone. It appears that N-protected covalent prodrugs

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::067a586e91114221712e1e44e5a1f912
https://doi.org/10.1021/jm980358u

Modelisation, Synthesis and Anti-HIV activities of N,N,N′,N″,N‴-pentakistetraazamacrocycles salts derivatives

Autor: M. Bouygues, Michel Camplo, Patrick Vlieghe, C. Trabaud, Jean-Louis Kraus, Jean Dessolin, Jean-Claude Chermann

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:1353-1358

The syntheses and the anti-HIV activities of new N,N,N′,N″,N‴-pentakistetraazamacrocyles salts analogues are described. From computer modeling studies, it was found that zinc coordination capacity of these pentakis derivatives was larger than t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4f89caf507bf575f1c2849a3cf897f80
https://doi.org/10.1016/s0960-894x(97)00222-9

Chemical optimization of new ligands of the low-density lipoprotein receptor as potential vectors for central nervous system targeting

Autor: Jean Martinez, Michel Khrestchatisky, Vincent Lisowski, Marion David, Franck Debarbieux, Patrick Vlieghe, Karima Abouzid, Aude Faucon, Nadine Payrot, Geneviève Rougon, Guillaume Jacquot, Nicolas Floquet, Jean-Daniel Malcor

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2012, 55 (5), pp.2227-41. ⟨10.1021/jm2014919⟩
Journal of Medicinal Chemistry, American Chemical Society, 2012, 55 (5), pp.2227-41. 〈10.1021/jm2014919〉
Journal of Medicinal Chemistry, 2012, 55 (5), pp.2227-41. ⟨10.1021/jm2014919⟩

International audience; Drug delivery to the central nervous system is hindered by the presence of physiological barriers such as the blood-brain barrier. To accomplish the task of nutrient transport, the brain endothelium is endowed with various tra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::611f4970f78d8beffc7c8e16e685d80d
https://hal.archives-ouvertes.fr/hal-00839126