N -Alkyl Urea Hydroxamic Acids as a New Class of Peptide Deformylase Inhibitors with Antibacterial Activity
نویسندگان
چکیده
منابع مشابه
Drug forecast – the peptide deformylase inhibitors as antibacterial agents
The relatively rapid development of microbial resistance after the entry of every new antimicrobial into the marketplace necessitates a constant supply of new agents to maintain effective pharmacotherapy. Despite extensive efforts to identify novel lead compounds from molecular targets, only the peptide deformylase inhibitors (PDIs) have shown any real promise, with some advancing to phase I hu...
متن کاملNew peptide deformylase inhibitors and cooperative interaction: a combination to improve antibacterial activity.
OBJECTIVES Bacterial drug resistance is a worrying public health problem and there is an urgent need for research and development to provide new antibacterial molecules. Peptide deformylase (PDF) is now a well-described intracellular target selected for the design of a new antibiotic group, PDF inhibitors (PDFIs). The initial bacterial susceptibility to an inhibitor of a cytoplasmic target is d...
متن کاملN-Heterocyclic analogues as peptide deformylase inhibitors: Molecular modeling, synthesis and antibacterial evaluation
Methods A new series of Nheterocyclic compounds has been derived from benzimidazole and pyrimidine nuclei optimized with the Discovery studio 3.0 software to investigate the interactions between the target compounds and the amino acid residues of Escherichia coli PDF Ni (PDB: ID 1G2A), and then synthesized. Further, all compounds were examined for their antibacterial activities against Gram-pos...
متن کاملMutagenicity and antibacterial activity of hydroxamic acids.
Hydroxamic acids demonstrated mutagenic and antibacterial activities. These activities appear to be dependent on the hydroxamic acid function and are probably due to the interaction with deoxyribonucleic acid.
متن کاملPeptide deformylase inhibitors as potent antimycobacterial agents.
Peptide deformylase (PDF) catalyzes the hydrolytic removal of the N-terminal formyl group from nascent proteins. This is an essential step in bacterial protein synthesis, making PDF an attractive target for antibacterial drug development. Essentiality of the def gene, encoding PDF from Mycobacterium tuberculosis, was demonstrated through genetic knockout experiments with Mycobacterium bovis BCG...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2002
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.46.9.2752-2764.2002