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Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives.
Molecules 2020; 25(2)M

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)).

Authors+Show Affiliations

Laboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, Senegal.Laboratoire de Chimie et Physique des Matériaux (LCPM), Université Assane SECK de Ziguinchor, Ziguinchor BP 523, Senegal.Centre National de Référence du Paludisme, Hôpital Bichat-Claude Bernard, APHP, 75018 Paris, France. Université Paris-Saclay, CNRS BioCIS, 92290 Châtenay-Malabry, France.Université Paris-Saclay, CNRS BioCIS, 92290 Châtenay-Malabry, France.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31940857

Citation

Seck, Rokhyatou, et al. "Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives." Molecules (Basel, Switzerland), vol. 25, no. 2, 2020.
Seck R, Gassama A, Cojean S, et al. Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives. Molecules. 2020;25(2).
Seck, R., Gassama, A., Cojean, S., & Cavé, C. (2020). Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives. Molecules (Basel, Switzerland), 25(2), doi:10.3390/molecules25020299.
Seck R, et al. Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives. Molecules. 2020 Jan 11;25(2) PubMed PMID: 31940857.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives. AU - Seck,Rokhyatou, AU - Gassama,Abdoulaye, AU - Cojean,Sandrine, AU - Cavé,Christian, Y1 - 2020/01/11/ PY - 2019/12/17/received PY - 2019/12/30/revised PY - 2020/01/10/accepted PY - 2020/1/17/entrez KW - antimalarial KW - drug lead KW - piperidine KW - reagent-based diversity KW - reductive amination JF - Molecules (Basel, Switzerland) JO - Molecules VL - 25 IS - 2 N2 - 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)). SN - 1420-3049 UR - https://www.unboundmedicine.com/medline/citation/31940857/Synthesis_and_Antimalarial_Activity_of_1,4-Disubstituted_Piperidine_Derivatives L2 - http://www.mdpi.com/resolver?pii=molecules25020299 DB - PRIME DP - Unbound Medicine ER -