Design and synthesis of a new class of 4-aminoquinolinyl- and 9-anilinoacridinyl Schiff base hydrazones as potent antimalarial agents

Abstract

A series of novel 4-aminoquinolinyl and 9-anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated in vitro for their antimalarial activity against chloroquine-sensitive strain 3D7 and the chloroquine-resistant K1 strain of P. falciparum and for cytotoxicity toward Vero cells. Compounds 17, 20, and 21 displayed good activity against the 3D7 strain with IC50 values ranging from 19.69-25.38 nM. Moreover, compounds 16, 17, 21, 24, 32 and 33 exhibited excellent activities (21.64-54.26 nM) against K1 strain and several compounds displayed β-hematin inhibitory activity, suggesting that, they act on the haem crystallization process like CQ. Compounds were also found to be nontoxic with good selectivity index