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Open AccessArticle

Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives

1
Laboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, Senegal
2
Centre National de Référence du Paludisme, Hôpital Bichat-Claude Bernard, APHP, 75018 Paris, France
3
Université Paris-Saclay, CNRS BioCIS, 92290 Châtenay-Malabry, France
*
Authors to whom correspondence should be addressed.
Molecules 2020, 25(2), 299; https://doi.org/10.3390/molecules25020299
Received: 17 December 2019 / Revised: 30 December 2019 / Accepted: 10 January 2020 / Published: 11 January 2020
(This article belongs to the Section Medicinal Chemistry)
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)). View Full-Text
Keywords: piperidine; reductive amination; reagent-based diversity; antimalarial; drug lead piperidine; reductive amination; reagent-based diversity; antimalarial; drug lead
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MDPI and ACS Style

Seck, R.; Gassama, A.; Cojean, S.; Cavé, C. Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives. Molecules 2020, 25, 299.

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