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

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

Volume: 11 Issue: 19

Author(s): Chitalu C. Musonda and Kelly Chibale

Affiliation:

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

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.

Cite this article as:

Musonda C. Chitalu and Chibale Kelly, Application of Combinatorial and Parallel Synthesis Chemistry Methodologies to Antiparasitic Drug Discovery, Current Medicinal Chemistry 2004; 11 (19) . https://dx.doi.org/10.2174/0929867043364469