Journal
PHARMACEUTICALS
Volume 15, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/ph15080999
Keywords
pharmaceuticals; tailor-made amino acids; fluorine; drug design; asymmetric synthesis
Categories
Funding
- National Natural Science Foundation of China [21761132021]
- IKERBASQUE, Basque Foundation for Science
- University of the Basque Country UPV/EHU [UFIQOSYC11/22]
- Basque Government (GVgrant) [IT1236-19]
- Ministerio de Ciencia e Innovacion [PID2019-109633GBC21]
Ask authors/readers for more resources
Nowadays, the selective introduction of fluorine into bioactive compounds is a mature strategy in drug design. Amino acids, on the other hand, are a ubiquitous class of organic compounds and have great potential in the development of targeted drugs. In recent years, there has been a clear trend in combining the structural features of both amino acids and fluorine in pharmaceutical design.
Nowadays, the selective introduction of fluorine into bioactive compounds is a mature strategy in the design of drugs allowing to increase efficiency, biological half-life and bio-absorption. On the other hand, amino acids (AAs) represent one of the most ubiquitious classes of naturally occurring organic compounds, which are found in over 40% of newly marked small-molecule pharmaceutical drugs and medical formulations. The primary goal of this work is to underscore two major trends in the design of modern pharmaceuticals. The first is dealing with the unique structural characteristics provided by the structure of amino acids featuring an abundance of functionality and the presence of a stereogenic center, all of which bodes well for the successful development of targeted bioactivity. The second is related to fine-tuning the desired activity and pharmacokinetics by selective introduction of fluorine. Historically, both trends were developed separately as innovative and prolific approaches in modern drug design. However, in recent decades, these approaches are clearly converging leading to an ever-increasing number of newly approved pharmaceuticals containing both structural features of amino acids and fluorine.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available