Peptide deformylase inhibitor containing 2, 5-dihydropyrrole and synthesizing method

Abstract

The invention provides a peptide deformylase inhibitor containing 2, 5-dihydropyrrole and a synthesizing method, which relates to a peptide deformylase inhibitor as well as a technique of preparing the same. The peptide deformylase inhibitor has the structure above, wherein in the formula R<1> is alkyl; R<2> is H or alkyl; R<3> is alkyl or aromatic radical or heterocycle. The peptide deformylase inhibitor provided by the invention can inhibit bacteria to synthesize protein, thereby killing bacteria, with small probability of drug tolerance and human body safety. The inhibitor can be used for killing diseased plant with drug tolerance to the existed antibiotic, such as: methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP) and enterococcus.The technique provided by the invention uses p-methoxy-benzyl hydroxylamine (PMBONH<2>) to substitute benzyl hydroxylamine (BnONH<2>) produced by other technologies, which enable removing protectiongroup to have better chemical selectivity, thereby finishing synthesis of a series of peptide deformylase inhibitors.

Description

technical field The invention discloses a peptide deformylase inhibitor containing 2,5-dihydropyrrole and a synthesis method thereof, relating to a peptide deformylase (PDF) inhibitor, and further relates to a preparation process of the inhibitor. The invention belongs to the technical field of antibiotics and antibacterial drugs. Background technique Antibiotics refer to microbial products (secondary metabolites) that can kill or inhibit some specific microorganisms such as bacteria, fungi, rickettsia, mycoplasma, chlamydia and viruses at high dilution. In 1929, British scholar Fleming first discovered penicillin among antibiotics. In 1940, based on Fleming's discovery, Florey and Chain invented penicillin for human injection. In 1944, Waksman isolated streptomycin. What is exciting is that this antibiotic has a strong resistance to Mycobacterium tuberculosis, making tuberculosis no longer a terminal disease. Since then, chloramphenicol (1947), neomycin (1949), oxytetrac...

AI Technical Summary

Problems solved by technology

As far as the current research situation is concerned, the chance of bacterial resistance to PDF inhibitors is very small

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