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CALDARELLI Sergio
Thème de Recherche: Nucléosides & Effecteurs Phosphorylés
sergio.caldarelli
univ-montp2.fr
Bureau: 0, Bât: 17 - Site : Faculté des sciences
Productions scientifiques :
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Exploring prodrug approaches for albitiazolium and its analogues.
Auteur(s): Peyrottes S., Caldarelli S., Wein Sharon, Perigaud C., Vial Henri
(Article) Publié:
Current Topics In Medicinal Chemistry, vol. 14 p.1653-1667 (2014)
Ref HAL: hal-01078458_v1
PMID 25116583
DOI: 10.2174/1568026614666140808121746
Résumé: 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 degradation in the food vacuole. This new and multiple mode of action is a major asset of these new class of antimalarials, as they could help delay resistance development. We synthesized and designed various sets of analogues, notably prodrugs, since the oral bioavailability of bis-thiazolium salts is relatively low. The chemistry underlying this synthesis relies on inexpensive and readily available starting materials and is straightforward. This is essential since the ultimate objective is to obtain affordable and orally available drugs for uncomplicated malaria treatment.
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Choline Analogues in Malaria Chemotherapy
Auteur(s): Peyrottes S., Caldarelli S., Wein Sharon, Perigaud C., Pellet Alain, Vial Henri
(Article) Publié:
Current Pharmaceutical Design, vol. 18 p.3454-3466 (2012)
Ref HAL: hal-00733161_v1
Résumé: 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 for the parasite, has thus been proposed as a novel and promising therapeutic strategy. This review compiles literature concerning the design and study of choline analogues and related cation derivatives as potential anti-malarials. It covers advances achieved over the last two decades and describes: the concept validation, the design and selection of a clinical candidate (Albitiazolium), back-up derivatives while also providing insight into the development of prodrug approaches.
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Exploration of potential prodrug approach of the bis-thiazolium salts T and T4 for orally delivered antimalarials.
Auteur(s): Caldarelli S., Boisbrun Michel, Alarcon Karine, Hamzé Abdallah, Ouattara Mahama, Salom-Roig X., Maynadier M., Wein Sharon, Peyrottes S., Pellet Alain, Calas M., Vial Henri J
(Article) Publié:
Bioorganic & Medicinal Chemistry Letters / Bioorganic And Medicinal Chemistry Letters, vol. 20 p.3953-3956 (2010)
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