Synthesis and Characterization of Phenylenediamine Side‐Chain‐Modified 4‐Aminoquinoline Mannich Bases and Evaluation of their in vitro Antimalarial Activity

Abstract

Twelve novel compounds (Phenylenediamine side chain modified 4‐Aminoquinoline Mannich Bases) were synthesized and characterized by using a variety of analytical and spectroscopic methods. All the synthesized compounds were screened for in‐vitro antimalarial activity on 3D7 strain of Plasmodium falciparum. Synthesized compounds showed MIC values between 1.9 and 125 μg/ml in antimalarial screening (in‐vitro). Two compounds (MIC=1.9 μg/ml or 1.953 0.10 μM and 7.8 μg/ml or 2.200 0.08 μM) were found most potent against chloroquine sensitive 3D7 strain of Plasmodium falciparum which is comparable to standard drug chloroquine (MIC=0.4 μg/ml or 0.106 0.01 μM).