Macrocycles: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry
International Pharmacy Acta,
Vol. 1 No. 1 (2018),
4 March 2018
,
Page 111-112
https://doi.org/10.22037/ipa.v1i1.20056
Abstract
Introduction: A cyclic compound is common motif in natural product structures. Cyclic peptides, a vast subset of natural products, display a wide variety of biological activities. Owing to their size, cyclic peptides are particularly attractive scaffolds for interrogating challenging biomolecular interactions, such as those at protein–protein interfaces.
Methods and Results:
This review takes an overview of the literature for the synthesis of peptide and non-peptide macrocycles, concentrating on advances in the last five years up to the end of 2017. These methods are clustered by strategies for preparation and further derivatization of preformed macrocycle-containing building blocks. Examples of the use of macrocycles in medicinal chemistry are reported, including a collation of macrocycle derivatives appearing in recent patents for medicinal chemistry applications.
Conclusions:
This review aims to provide an overview of the extensive recent studies involving macrocycles in synthesis and medicinal chemistry and to highlight the continuing challenges.
- Macrocycle; Peptide; Human Programmed Death 1; biomolecular
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