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Updated: Dec 30, 2025

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives
Rokhyatou Seck1, Abdoulaye Gassama1, Sandrine Cojean2,3
1Laboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, Senegal.
Abstract:
In order to prepare, at low cost, new compounds active against Plasmodium falciparum, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives 6. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of P. falciparum. The most active molecules-compounds 12d (13.64 nM (3D7)), 13b (4.19 nM (3D7) and 13.30 nM (W2)), and 12a (11.6 nM (W2))-were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)).
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