ApplicationofBioisosteresinDrugDesign

Literature Seminar Yuya Morita (M1). Application of Bioisosteres in Drug Design O O. H F. N N. O. N. N. OH. H. Contents 1. Introduction ~What are Bioisosteres? ~Drug-like Concepts 2. Application of Isosteres in Drug Design ~Fluorine as an Isostere of Hydrogen ~Carboxylic Acid Isosteres ~Phenol Isosteres ~Amide and Ester Isosteres ~Phenyl Ring Isosteres 3. Oxetanes in Drug Discovery ~Physicochemical Properties of Oxetanes ~Oxetanes as Isosteres ~Preparation of Oxetanes 4. Summary 1. Introduction What are bioisosteres? Isostere The isostere concept was formulated by Irving Langmuir in 1919. J. Am. Chem. Soc. 1919, 41, 1543. The octet theory of valence indicates that if compounds having the same number of atoms have also the same total number of electrons, the electrons may arrange themselves in the same manner.

2.ApplicationofIsosteresinDrugDesign FluorineasanIsostereofHydrogen The unique properties of fluorine have led to its widespread application in drug design as an

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