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

Author: Egan T.J.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 1, May 2001 , pp. 113-123(11)

Publisher: Bentham Science Publishers

Buy & download fulltext article:

Price: $63.10 plus tax (Refund Policy)

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

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557013407188

Publication date: 2001-05-01

More about this publication?

The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.