Exploring Prodrug Approaches for Albitiazolium and its Analogues

Autor: Suzanne Peyrottes, Henri Vial, Sergio A. Caldarelli, Sharon Wein, Christian Périgaud

Publikováno v: Current Topics in Medicinal Chemistry
Current Topics in Medicinal Chemistry, Bentham Science Publishers, 2014, 14 (14), pp.1653-1667. ⟨10.2174/1568026614666140808121746⟩

International audience; Choline analogues such as bis-thiazolium salts are thought to inhibit choline transport into Plasmodiuminfected erythrocytes, thus preventing parasite PC biosynthesis, and also to interact with plasmodial haemoglobin degradati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb7408e127d9a95be880995248e24cb4
https://doi.org/10.2174/1568026614666140808121746

Exploration of potential prodrug approach of the bis-thiazolium salts T3 and T4 for orally delivered antimalarials

Autor: Michel Boisbrun, Henri Vial, Suzanne Peyrottes, Karine Alarcon, Michèle Calas, Xavier J. Salom-Roig, Marjorie Maynadier, Mahama Ouattara, Sergio A. Caldarelli, Sharon Wein, Alain Pellet, Abdallah Hamze

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:3953-3956

We report here the synthesis and biological evaluation of a series of 37 compounds as precursors of potent antimalarial bis-thiazolium salts (T3 and T4). These prodrugs were either thioester, thiocarbonate or thiocarbamate type and were synthesized i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bed51e92aaa4c1d32c60044f9d758ca9
https://doi.org/10.1016/j.bmcl.2010.05.001

New Bis-thiazolium Analogues as Potential Antimalarial Agents: Design, Synthesis, and Biological Evaluation

Autor: Suzanne Peyrottes, Siham El Fangour, Alain Pellet, Christian Périgaud, Christophe Tran Van Ba, Sergio A. Caldarelli, Sharon Wein, Henri Vial

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2013, 56, pp.496-509. ⟨10.121/jm3014585⟩

International audience; Bis-thiazolium salts are able to inhibit phosphatidylcholine biosynthesis in Plasmodium and to block parasite proliferation in the low nanomolar range. However, due to their physicochemical properties (i.e., permanent cationic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76d27e2b3ca72b68119a73c12cbbd318
https://hal.archives-ouvertes.fr/hal-00783503

Choline Analogues in Malaria Chemotherapy

Autor: Suzanne Peyrottes, Sergio A. Caldarelli, Sharon Wein, Christian Périgaud, Alain Pellet, Henri Vial

Publikováno v: Current Pharmaceutical Design
Current Pharmaceutical Design, Bentham Science Publishers, 2012, 18 (24), pp.3454-3466. ⟨10.2174/138161212801327338⟩

International audience; Emerging resistance against well-established anti-malaria drugs warrants the introduction of new therapeutic agents with original mechanisms of action. Inhibition of membrane-based phospholipid biosynthesis, which is crucial f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1a933e13a455172c8bb3b2165ede22a
https://hal.archives-ouvertes.fr/hal-00733161

Short peptide nucleic acids (PNA) inhibit hepatitis C virus internal ribosome entry site (IRES) dependent translation in vitro

Autor: Sergio A. Caldarelli, Christine Alotte, David Durantel, Amaury Martin, Olivier Hantz, Fabien Zoulim, Roger Condom, Audrey Di Giorgio

Publikováno v: Antiviral research. 80(3)

The internal ribosome entry site (IRES) of hepatitis C virus (HCV) which governs the initiation of protein synthesis from viral RNA represents an ideal target for antisense approaches. Using an original bicistronic plasmid, we first established that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de0e536214294e316b996f732aec63be
https://pubmed.ncbi.nlm.nih.gov/18625270