Royo, Santiago published the artcileDipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action, Safety of (S)-4-Benzylthiazolidine-2-thione, the main research area is dipeptidyl enoate derivative preparation rhodesain inhibitor trypanosomicides; dipeptidyl enoates; inhibitors; rhodesain; sleeping sickness; trypanosomiasis.
Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-Et 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nΜ and kinact/Ki=1.6×106 Μ-1 s-1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations Inhibition kinetics data, supported by docking studies, suggest a dual mode of action via attack of cysteine thiolate at two reactive positions.
ChemMedChem published new progress about Enzyme inhibitors (rhodesain). 171877-39-7 belongs to class thiazole, name is (S)-4-Benzylthiazolidine-2-thione, and the molecular formula is C10H11NS2, Safety of (S)-4-Benzylthiazolidine-2-thione.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica