Structure–activity relationships for ferriprotoporphyrin IX association and β-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods

S Nsumiwa, D Kuter, S Wittlin, K Chibale…

Index: Nsumiwa, Samkele; Kuter, David; Wittlin, Sergio; Chibale, Kelly; Egan, Timothy J. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 13 p. 3738 - 3748

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Citation Number: 6

Abstract

In order to probe structure–activity relationships of association with ferriprotoporphyrin IX (logK) and inhibition of β-hematin formation, a series of 4-aminoquinolines with varying substituents at the 7-position (X) have been synthesized. These have been further elaborated by introduction of two different R groups on the 4-amino nitrogen atom in the form of methyl (R= Me) and ethylamine (R= EtNH2) side chains. Data for a previously ...