01658nas a2200169   4500008004100000022001400041245010400055210006900159260000900228300001400237490000700251520102100258100002301279700002901302700002601331856013101357       2025                        eng d  a1523-706000aPeptide functionalization with dithioate and trithioate groups: A CS2-mediated solid-phase approach0 aPeptide functionalization with dithioate and trithioate groups A  cMAY   a6271-62780 v273 a<p>
	The dithiocarbamate group is an important class of compounds whose presence in small molecules and peptides leads to antimicrobial, anticancer, and enzyme inhibition properties. This study introduces an efficient and selective method for incorporating dithioate and trithioate moieties into amino acids and peptides using CS2 chemistry under mild conditions. Utilizing a N,N-diisopropylethylamine (DIPEA)-CS2-benzyl chloride system, we achieved modifications at the N-terminal amines and the side chains of Lys and Cys residues through solid-phase peptide synthesis (spps). The method exhibits excellent yields and broad compatibility with diverse amino acids, their protection groups, peptide chemistry reagents, and varied peptide sequences. Notably, the successful incorporation of trithioate groups into peptides via cysteines, reported here for the first time, expands the functional repertoire of peptide chemistry, offering new possibilities for peptide-based drug design and related applications.</p>
1 aShinde, Dinesh, R.1 aBodake, Supriya, Mahadev1 aMarelli, Udaya, Kiran  uhttps://library.ncl.res.in/content/peptide-functionalization-dithioate-and-trithioate-groups-cs2-mediated-solid-phase-approach