Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum

MO Anderson, J Sherrill, PB Madrid, AP Liou…

Index: Anderson, Marc O.; Sherrill, John; Madrid, Peter B.; Liou, Ally P.; Weisman, Jennifer L.; DeRisi, Joseph L.; Guy, R. Kiplin Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 2 p. 334 - 343

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Citation Number: 54

Abstract

A parallel synthetic strategy to the 9-aminoacridine scaffold of the classical anti-malarial drug quinacrine (2) is presented. The method features a new route to 9-chloroacridines that utilizes triflates of salicylic acid derivatives, which are commercially available in a variety of substitution patterns. The route allows ready variation of the two diversity elements present in this class of molecules: the tricyclic aromatic heterocyclic core, and the disubstituted ...