Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum

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• 作者：Koneni V. Sashidhara ; Srinivasa Rao Avula ; Gopala Reddy Palnati ; Shiv Vardan Singh ; Kumkum Srivastava ; Sunil K. Puri ; J.K. Saxena
• 关键词：Synthesis ; Quinoline ; Chalcones ; Antimalarial agents
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 September, 2012
• 年：2012
• 卷：22
• 期：17
• 页码：5455-5459
• 全文大小：1342 K

文摘

The control of malaria has been complicated with increasing resistance of malarial parasite against existing antimalarials. Herein, we report the synthesis of a new series of chloroquine-chalcone based hybrids (8-22) and their antimalarial efficacy against both chloroquine-susceptible (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. Most of the compounds showed enhanced antimalarial activity as compared to chloroquine in chloroquine-resistant (K1) strain of Plasmodium falciparum. Furthermore, to unfold the mechanism of action of these synthesized hybrid molecules, we carried out hemin dependent studies, in which three compounds were found to be active.