Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Macrocycles occupy a unique segment of chemical space. In the past decade, their chemical
diversity expanded significantly, supported by advances in bioinformatics and synthetic …

An increasingly large number of bioactive cyclic peptides have been found in nature. The
enhanced biological specificity, activity, and metabolic stability of cyclopeptides, by virtue of …

A two-step sequence involving an Ugi four-component reaction and an intramolecular
nucleophilic aromatic substitution (SNAr) has been developed for the rapid access to biaryl …

From readily accessible starting materials, macrocycles with an endo aryl− aryl ether bond
are synthesized in only two operations by combination of the Ugi four-component reaction …

Differentiation of the physiological role of the melanocortin receptor 5 MC5R from that of
other melanocortin receptors will require development of high affinity and selective …

Solid-phase synthesis of natural product-like macrocycles by a sequence of Ugi-4CR and
SNAr-based cycloetherification - ScienceDirect Skip to main contentSkip to article Elsevier …

On-resin SNAr reactions were performed to prepare the macrocyclic β-turn mimics 1a− n
(Scheme 1 and Table 1). These reactions occurred more efficiently than completely …

A new method to access cyclic peptidomimetics via a Pd-catalyzed macroamination reaction
is presented. Natural amino acid amines are revealed as proficient coupling partners in …

While a range of strategies exist to accomplish peptide macrocyclization, they are frequently
limited by the need for orthogonal protection or provide little opportunity for structural …