Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors

The synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated to discover SAR at P1′ and P3′ positions, and most of these derivatives exhibit better in vitro antibacterial activity than existing drugs against drug-resistant clinical isolates including MRSA, PRSP, and Haemophilus influenzae.

Graphical abstractDesign and synthesis of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors, and their antibacterial activities against susceptible and resistant clinical isolates including Gram-positive bacterial strains and Gram-negative ones have been reported.Figure optionsDownload full-size imageDownload as PowerPoint slide