Chapter 4 - Primary, Secondary and Tertiary Amines and their Isosteres
Identifieur interne : 001649 ( Main/Exploration ); précédent : 001648; suivant : 001650Chapter 4 - Primary, Secondary and Tertiary Amines and their Isosteres
Auteurs : D. K. Walker [Royaume-Uni] ; R. M. Jones [Royaume-Uni] ; A. N. R. Nedderman [Royaume-Uni] ; P. A. Wright [Royaume-Uni]Source :
- RSC Drug Discovery [ 2041-3203 ]
Abstract
Amines are one of the most well represented functional groups amongst small drug molecules. These compounds cover a wide range of therapeutic applications and possess a broad spectrum of physicochemical properties. In the majority of cases the amine provides a positively charged function that is important for interaction with the target receptor. The ionised amine function is also capable of ion pair interactions with other entities such as the ionised head group of membrane phospholipids, the active site of a number of transporter proteins and the active site of certain drug metabolising enzymes (e.g. CYP2D6). These give distinct distribution , excretion and metabolism patterns. Furthermore the electronic characteristics of the nitrogen atom render it facile to many oxidative enzymatic processes, making the amine function pivotal to the metabolism of many of the representatives of drugs incorporating this functionality.
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DOI: 10.1039/9781849731102-00168
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