ChemInform Abstract: Medicinal Chemistry of α-Hydroxy-β-amino Acids

ChemInform ◽  
2012 ◽  
Vol 43 (25) ◽  
pp. no-no
Author(s):  
Zyta Ziora ◽  
Mariusz Skwarczynski ◽  
Yoshiaki Kiso
Author(s):  
Zyta Ziora ◽  
Mariusz Skwarczynski ◽  
Yoshiaki Kiso

2021 ◽  
Vol 25 ◽  
Author(s):  
Jianlin Han ◽  
Hiroyuki Konno ◽  
Tatsunori Sato ◽  
Kunisuke Izawa ◽  
Vadim A. Soloshonok

: Amino acids (AAs) play an important role in modern health industry. AAs’ residues are frequently found in the structures of small-molecule modern pharmaceuticals, while peptidomimetics and peptide-based drugs are entirely derived from AAs. The goal of this review article is to highlight that, currently, AAs serve as key structural features in numerous successful pharmaceuticals; they are the so-called blockbuster drugs. In this work, we provide a detailed profile of 5 peptidomimetics and 4 peptide drugs. For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.


Symmetry ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 558 ◽  
Author(s):  
Elena Lenci ◽  
Andrea Trabocchi

Natural and nonnatural amino acids represent important building blocks for the development of peptidomimetic scaffolds, especially for targeting proteolytic enzymes and for addressing protein–protein interactions. Among all the different amino acids derivatives, proline is particularly relevant in chemical biology and medicinal chemistry due to its secondary structure’s inducing and stabilizing properties. Also, the pyrrolidine ring is a conformationally constrained template that can direct appendages into specific clefts of the enzyme binding site. Thus, many papers have appeared in the literature focusing on the use of proline and its derivatives as scaffolds for medicinal chemistry applications. In this review paper, an insight into the different biological outcomes of d-proline and l-proline in enzyme inhibitors is presented, especially when associated with matrix metalloprotease and metallo-β-lactamase enzymes.


2020 ◽  
Vol 103 ◽  
pp. 104236 ◽  
Author(s):  
Özlem Akgül ◽  
Andrea Angeli ◽  
Daniela Vullo ◽  
Fabrizio Carta ◽  
Claudiu T. Supuran

Amino Acids ◽  
2005 ◽  
Vol 29 (2) ◽  
pp. 89-100 ◽  
Author(s):  
A. Kuhl ◽  
M. G. Hahn ◽  
M. Dumić ◽  
J. Mittendorf

2021 ◽  
Author(s):  
Raj K Tak ◽  
Fuyuki Amemiya ◽  
Hidetoshi Noda ◽  
Masakatsu Shibasaki

The advent of saturated N-heterocycles as valuable building blocks in medicinal chemistry has led to the development of new methods to construct such nitrogen-containing cyclic frameworks. Despite the apparent strategic...


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