Exploring Prodrug Approaches for Albitiazolium and its Analogues

Title:Exploring Prodrug Approaches for Albitiazolium and its Analogues

Volume: 14 Issue: 14

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

Affiliation:

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

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.

Cite this article as:

Peyrottes Suzanne, Caldarelli Sergio, Wein Sharon, Perigaud Christian and Vial Henri, Exploring Prodrug Approaches for Albitiazolium and its Analogues, Current Topics in Medicinal Chemistry 2014; 14 (14) . https://dx.doi.org/10.2174/1568026614666140808121746