Design, synthesis and evaluation of 4-aminoquinoline-purine hybrids as potential antiplasmodial agents

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• 作者：P. Linga Reddy^a ; Shabana I. Khan^b ; Prija Ponnan^a ; Mohit Tripathi^a ; Diwan S. Rawat^a ; ^{dsrawat@chemistry.du.ac.in}
• 关键词：Antimalarial hybrids ; Aminoquinoline ; Antiplasmodial activity ; Heme binding activity ; Docking studies
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：675-686
• 全文大小：1767 K
• 卷排序：126

文摘

A series of novel 4-aminoquinoline-purine hybrids was synthesized. Potent antiplasmodial activity against CQ-sensitive and CQ-resistant strains. Up to six-fold better activity than reference drug (CQ) against resistant strain. Mechanistic heme-binding studies showed 1:1 binding stoichiometry. Computational docking studies with HGPRT protein revealed good binding interactions.