The present invention provides a
benzofuran compound, a preparation method and applications thereof, wherein the structure is represented by a general formula (I-1) or (I-2), R1, R3 and R4 are any one selected from
hydrogen, C1-C5 straight or branched chain
alkyl, hydroxyl, an
aldehyde group, an acetyl group, a carboxyl group, a cyano group, an amino group, a nitro group,
fluorine,
chlorine,
bromine, an
amide group, an ester group, an
alkoxy group, an aromatic group, and a heteroaromatic group, R2 is any one selected from
hydrogen, C1-C5 straight or branched chain
alkyl group, a hydroxyl group, an aromatic group, and a heteroaromatic group, and m and n are integers of 0-5. According to the present invention, the
Staphylococcus aureus
protease Sortase A substrate polypeptide fragment -LPXTG- is adopted as the structural
simulation object, the
benzofuran structure is adopted as the
simulation substrate
proline, and the linked
amide hydrophobic fragment segment is used to stimulate the substrate
leucine residue to design the novel
protease Sortase A inhibitor.