World Journal of
Pharmaceutical and Life Sciences

SYNTHESIS AND EVALUATION OF QUINOLINE AND PIPERIDINE DERIVATIVES AS EHMT2 INHIBITORS: PROSPECTS FOR ANTIMALARIAL DRUG DEVELOPMENT

Moussa Toure, Oumar Sambou, Abdoulaye Gassama*, Christian Cave and Sandrine Cojean

ABSTRACT

In this study, we report the synthesis of a set of quinoline and piperidine derivatives and the in vitro evaluation of their antimalarial activity against chloroquine-sensitive (Pf3D7) and chloroquine-resistant (PfW2) P. falciparum strains. The in vitro cytotoxicity of these compounds was assessed to determine their impact on human cells. Preliminary in vitro results showed that these compounds displayed selective cytotoxicity and potent activity against both strains. In particular, compound 8 showed promising activity, with CI50 values of 1.36 ?M for strain 3D7 and 6.57 ?M for strain W2. An in silico approach was used in parallel, such as molecular docking and pharmacological and pharmacokinetic properties prediction (ADME) to study the ability of these compounds to bind to the target of interest and to predict their efficacy and safety in the context of oral administration.

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