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

Wei Shi; Haikun Ma; Yuejiao Duan; Kelly Aubart; Yuhong Fang; Rimma Zonis; Liping Yang; Wenhao Hu

doi:10.1016/j.bmcl.2010.11.102

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

Bioorg Med Chem Lett. 2011 Feb 1;21(3):1060-3. doi: 10.1016/j.bmcl.2010.11.102. Epub 2010 Nov 30.

Authors

Wei Shi¹, Haikun Ma, Yuejiao Duan, Kelly Aubart, Yuhong Fang, Rimma Zonis, Liping Yang, Wenhao Hu

Affiliation

¹ Institute of Drug Discovery and Development, Department of Chemistry, East China Normal University, Shanghai, China.

PMID: 21185180
DOI: 10.1016/j.bmcl.2010.11.102

Abstract

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 P(1') and P(3') 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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amidohydrolases / antagonists & inhibitors*
Amidohydrolases / metabolism
Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology
Drug Design
Drug Resistance, Bacterial / drug effects
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Haemophilus influenzae / drug effects
Methicillin-Resistant Staphylococcus aureus / drug effects
Microbial Sensitivity Tests
Pyrrolidines / chemical synthesis
Pyrrolidines / chemistry*
Pyrrolidines / pharmacology

Substances

Anti-Bacterial Agents
Enzyme Inhibitors
Pyrrolidines
Amidohydrolases
peptide deformylase
pyrrolidine