Design and Synthesis of a New Class of 4-Aminoquinolinyl- and 9-Anilinoacridinyl Schiff Base Hydrazones as Potent Antimalarial Agents

作者：Sharma Moni; Chauhan Kuldeep; Srivastava Rajeev K; Singh Shiv V; Srivastava Kumkum; Saxena Jitendra K; Puri Sunil K; Chauhan Prem M S^*

来源：Chemical Biology & Drug Design, 2014, 84(2): 175-181.

DOI：10.1111/cbdd.12289

• 4-aminoquinoline
• 9-anilinoacridine
• antimalarial
• oxalamide
• Schiff base

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 Plasmodium 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 to 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 beta-hematin inhibitory activity, suggesting that they act on the heme crystallization process such as CQ. Compounds were also found to be non-toxic with good selectivity index.

• 出版日期2014-8