Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: Structure-Function Relationships in Chloroquine and Related 4-Aminoquinoline Antimalarials
Volume: 1 Issue: 1
Author(s): Timothy J. Egan
Affiliation:
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
Abstract: 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.
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Cite this article as:
Egan J. Timothy, Structure-Function Relationships in Chloroquine and Related 4-Aminoquinoline Antimalarials, Mini-Reviews in Medicinal Chemistry 2001; 1 (1) . https://dx.doi.org/10.2174/1389557013407188
DOI https://dx.doi.org/10.2174/1389557013407188 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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