Historically, natural products have great relevance for the development of new drugs. Natural molecules, in addition to directly providing new compounds with different therapeutic functions have provided scaffolds and a great diversity of structures that serve as inspiration for the design and discovery of new drugs. The great structural complexity and the significant number of natural compounds that can be obtained and their advantages also present some historical problems that need to be overcome. Issues such as difficulty in isolation, difficulty in synthesizing compounds found in nature in the laboratory, screening to evaluate the biological properties of these compounds, and structural optimization to enhance the pharmacological properties of biomolecules; are some of the main difficulties encountered in research with natural products and in the design/discovery of new medicines. Therefore, this book addresses the great scientific advances that provide practical solutions to using natural products to develop new drugs. We address topics related to the genesis of research projects that use natural products to design new drugs. We address the discovery of new species, initial processes for identification and extraction of compounds, isolation and identification of these structures, techniques, and advances in vitro and in vivo methods that support the discovery of new natural drugs, synthesis of new compounds from natural molecules, in silico optimization processes of potentially promising compounds.