Exploring Prodrug Approaches for Albitiazolium and its Analogues

Author(s): Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud, Henri Vial.

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 14 , 2014

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Abstract:

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.

Keywords: Antimalarials, choline analogues, phospholipid, plasmodium, prodrugs, thiazolium salts.

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Article Details

VOLUME: 14
ISSUE: 14
Year: 2014
Page: [1653 - 1667]
Pages: 15
DOI: 10.2174/1568026614666140808121746
Price: $58

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