>>> Properties & Applications <<<

Cycloalkyl-substituted amino acids replace the branched isopropyl group of valine with an aliphatic ring formed through one or more carbon or heteroatom linkages, giving rise to cyclic or bridged side chains.

Such structures provide a constrained alternative for tuning the size, hydrophobicity, and spatial arrangement of amino acid residues.
As one example, during the optimization of a SARS-CoV-2 Mpro inhibitor, replacing a valine residue with a cyclopentyl-substituted amino acid improved SARS-CoV-2 Mpro inhibitory activity, with the IC50 decreasing from 0.0245 ± 0.00 to 0.011 ± 0.002 μM.
Further optimization of other structural elements ultimately afforded a potent orally bioavailable SARS-CoV-2 Mpro inhibitor.

[More info] 📰http://doi.org/10.1021/acs.jmedchem.5c00581

>>> Available Building Blocks <<<

CLICK IMAGE to try BLD Pharm's Cycloalkyl-Substituted Amino Acids 👆 in your research,

📧 or contact [email protected] for any inquiries.