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

Molecules

Sandrine Cojean¹  Rokhyatou Seck²  Abdoulaye Gassama²  Christian Cavé³ 

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

关键词: piperidine;    reductive amination;    reagent-based diversity;    antimalarial;    drug lead;   

DOI  :  10.3390/molecules25020299

来源: DOAJ

【 摘 要 】

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)).

【 授权许可】

Unknown