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Application of Combinatorial and Parallel Synthesis Chemistry Methodologies to Antiparasitic Drug Discovery

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Abstract:

The discovery and development of novel drugs has been influenced over the last several decades by new techniques in medicinal chemistry. Combinatorial and parallel synthesis chemistry techniques have opened up immense opportunities in drug discovery and development efforts. These techniques, which include solid phase organic synthesis and polymer-assisted synthesis in solution, have been routinely applied to a number of therapeutic areas. Despite the flurry of activity that characterized small molecule drug discovery efforts in the early 1990s, it was only during the mid to late 1990s that combinatorial chemistry began to make an impact on antiparasite chemotherapy. This review focuses on the development and application of combinatorial and parallel synthesis methodologies to antiparasitic drug discovery from the mid 1990s to the end of 2002. Much of this work applies to small organic molecules as inhibitors of parasite targets although some of the early applications were to the synthesis of enzyme substrates.

Keywords: antimalarial; antiparasitic drugs; combinatorial chemistry; parallel synthesis; polyaminebased derivatives; solid phase organic synthesis; trypanothione

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867043364469

Affiliations: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.

Publication date: October 1, 2004

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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