Structure-Function Relationships in Chloroquine and Related 4-Aminoquinoline Antimalarials

Author(s): Timothy J. Egan

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 1 , Issue 1 , 2001

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Recent publications have provided strong evidence that activity and cellular uptake of 4-aminoquinoline antimalarials depends on vacuolar haemoglobin degradation and that haematin is the drug target. Studies on haematin-quinoline interactions have provided insight into the structural requirements for these interactions and indications are that 4-aminoquinolines may act by inhibiting haemozoin formation. Structural requirements for this activity have also been reported recently and have led to construction of an empirical structure-function relationship for 4-aminoquinolines.

Keywords: Aminoquinoline Antimalarials, haematin quinoline interactions, plasmepsins, oxidative assault, parasitised red cells, haemoglobin degradation, DMSO complexes, coplanar interaction, amodiaquine analogue tebuquine, haem-polymerase, vacuolar pH

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Article Details

Year: 2001
Page: [113 - 123]
Pages: 11
DOI: 10.2174/1389557013407188

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