Integration of Synthetic Organic Chemistry and <i>in silico</i> Drug Discovery - Lead Discovery of Renin Inhibitors and <i>O</i>-GlcNAcase Inhibitors

Synthetic organic chemistry is a core technology of drug discovery, but combined with in silico technology which consists of molecular modeling and/or informatics using computational methods, it can be expected to accelerate drug discovery research and increase the success rate for developing a new drug. However, in silico technology cannot create new drugs by itself, and its integration with organic chemistry is necessary. In this paper, we describe drug discovery research that effectively integrates organic chemistry and in silico technology to develop synthetic strategies and efficiently create a novel lead compound or in vivo tool.