title: "Drug" Discovery with the Help of Organic Chemistry.
abstract: The first step in "drug" discovery is to find compounds binding to a potential drug target. In modern medicinal chemistry, the screening of a chemical library, structure-based drug design, and ligand-based drug design, or a combination of these methods, are generally used for identifying the desired compounds. However, they do not necessarily lead to success and there is no infallible method for drug discovery. Therefore, it is important to explore medicinal chemistry based on not only the conventional methods but also new ideas. So far, we have found various compounds as drug candidates. In these studies, some strategies based on organic chemistry have allowed us to find drug candidates, through 1) construction of a focused library using organic reactions and 2) rational design of enzyme inhibitors based on chemical reactions catalyzed by the target enzyme. Medicinal chemistry based on organic chemical reactions could be expected to supplement the conventional methods. In this review, we present drug discovery with the help of organic chemistry showing examples of our explorative studies on histone deacetylase inhibitors and lysine-specific demethylase 1 inhibitors.
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine.
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
mesh_terms: D002625:Chemistry, Organic; D055808:Drug Discovery / Q000379:methods* / Q000639:trends*; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D056466:Histone Demethylases / Q000037:antagonists & inhibitors; D055601:Organic Chemistry Phenomena
chemical_list: D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D056466:Histone Demethylases; C495195:KDM1A protein, human