β-Proline Scaffold

Compared to traditional α-amino acid designs, constructing bioactive molecules using β-amino acids offers several advantages, such as increased resistance to endogenous proteases, which enhances metabolic stability. Among those, β-proline has emerged as a particularly promising molecular framework, serving as the basis for multiple drugs in clinical trials. Its conformational rigidity facilitates preorganized interactions with targets, while its multiple substitution sites allow for precise modulation of molecular volume and pharmacological properties.

β-Proline Scaffold