The exploration of privileged structures in drug discovery is a rapidly emerging theme in
medicinal chemistry. These structures represent a class of molecules capable of binding to …

Unnatural α-amino acids form a family of essential molecules used for, among other
applications, the synthesis of modified peptides, to improve resistance to proteolytic enzyme …

Organic molecules as well as metal complexes may exist as several geometric isomers1
which display distinct physical properties and chemical reactivities. A molecule containing …

The amide bond is one of the most important functional groups in chemistry and biology. 1
Due to the strong resonance interaction between nN and π* C O orbitals (Figure 1), 2 the …

Hydroxytryptamine type 3 (5-HT3) receptors are members of the Cys-loop receptor
superfamily. Neurotransmitter binding in these proteins triggers the opening (gating) of an …

Head-to-tail cyclic peptides have been reported to bind to multiple, unrelated classesof
receptor with high affinity. They may therefore be considered to beprivileged structures. This …

Non-proteinogenic prolines have been acknowledged as an important pool for the synthesis
of conformationally rigid bioactive peptides, angiotensin converting enzyme inhibitors and …

Amide bonds at the proline nitrogen are particularly susceptible to rotation, affording cis and
trans isomers. Installation of a stereochemically defined electron-withdrawing fluorine atom …

We examine the relationship between covalent structure and conformational propensity
among a series of β-amino acid tetramers. These experiments focus on the hairpin folding …

Conformationally constrained amino acid and dipeptide units can serve in mimics of specific
secondary structures for studying relationships between peptide conformation and biological …