1.10 Chirality and Combinatorial Libraries for Drug Discovery, an Overview

This chapter outlines the major accomplishments and recent developments in the area of combinatorial libraries composed of chiral molecules. Examples presented in this chapter largely focus on the process of early drug discovery, with a particular focus on natural product (NP)-like scaffolds and small organic molecules. Accordingly, hit-to-lead finding approaches are the main focus of this study. The topic of combinatorial biocatalysis has also been included in this chapter as it represents a powerful and useful direction in the synthesis of chiral libraries.