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In enzymology, a peptide deformylase (EC 3.5.1.88) is an enzyme that catalyzes the chemical reaction formyl-L-methionyl peptide + H₂O ⇌ formate + methionyl peptide Thus, the two substrates of this enzyme are formyl-L-methionyl peptide and H₂O, whereas its two products are formate and methionyl peptide. This enzyme belongs to the family of hydrolases, those acting on carbon-nitrogen bonds other than peptide bonds, specifically in linear amides.
A 1,3,4-thiadiazole peptide deformylase enzyme inhibitor and preparation and application thereof
This invention relates to a 1,3,4-thiadiazole peptide deformylase inhibitor and its preparation and application. The structural formula is shown in formula (1): wherein, R 1 It is n-butyl or cyclopentylmethyl; R 2 The compounds are hydrogen-containing, straight-chain alkanes, cyclic alkanes, aromatic rings, substituted biphenyls, or heterocyclic rings. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention can effectively inhibit bacterial protein synthesis, thereby achieving sterilization. These compounds exhibit excellent inhibitory activity against Gram-positive drug-resistant bacteria, especially the clinically challenging methicillin-resistant Staphylococcus aureus (MRSA). In particular, some preferred compounds show inhibitory activity 4-8 times that of the control standards vancomycin and linezolid. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention also exhibit inhibitory activity against Gram-negative drug-resistant bacteria, especially against drug-resistant Acinetobacter baumannii, known as "superbugs," with an inhibitory activity reaching 0.5 μg / mL, far superior to vancomycin and linezolid.
Owner:SHANGHAI UNIV