ABSTRACT
Stereochemically and functionally rich natural products are abundantly present in all organisms and are essential ingredients for all life. The influence of natural products in the discovery of new marketed therapeutics continues to be significant in various therapeutic areas. Although the biological machinery in the living organisms generates natural products, synthetic chemistry is the primary method used by the pharmaceutical industry for generating natural product-based molecules. Another approach is the use of multicomponent reactions to rapidly and efficiently construct structurally complex and varied polycyclic natural product-like compounds. Combinatorial chemistry grew in the 1990s as a technology-based solution to the demand for compounds in the high-throughput screening campaigns against various therapeutic targets. Although a significant number of biologically active compounds have been generated by the combinatorial chemistry, the field continues to be criticized for its inability to generate leads and drugs.
