1. 2-Heteroarylethylamines in medicinal chemistry: a review of 2-phenethylamine satellite chemical space
- Author
-
Carlos Nieto, Alejandro Manchado, Ángel García-González, David Díez, and Narciso M. Garrido
- Subjects
bioisosteres ,2-heteroarylethylamines ,medicinal chemistry ,2-phenethylamine ,scaffold hopping ,Science ,Organic chemistry ,QD241-441 - Abstract
The concept of bioisostere replacement is of paramount importance in medicinal chemistry, as it can be employed as a rational to expand bioactive chemical space to tackle lead optimization issues like lack of potency, efficacy, and selectivity or pharmacokinetic/dynamic issues. One of the most important building blocks (in the sense of participating in a vast area of chemical space of biological importance) in medicinal chemistry is the 2-phenethyl moiety, a key component of diverse drug-like entities. Although the core 2-phenethylamine structure has been recognized by the drug discovery community, little attention has been given to the various ring-based rescaffolding procedures that can be conducted with this unit. In this regard, a review on the use of 2-heteroarylethylamines displaying pharmacological activity is reported. A detailed description of flexible, amine-opened motifs is provided, that describes therapeutic targets and other potent bioactive examples, which will be a valuable repository of phenyl, heteroaryl, and other replacement units of high value to the drug discovery community.
- Published
- 2024
- Full Text
- View/download PDF