[4.3.0] pyrazolidinones as potential antibacterial agents |
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| Affiliation: | 1. Research Service, Louis Stokes Cleveland Department of Veterans Affairs Medical Center, Cleveland, OH, 44106, USA;2. Department of Biochemistry, Case Western Reserve University, Cleveland, OH, 44106, USA;3. Yale Center for Molecular Discovery, West Haven, CT, 06516, USA;4. Department of Medicine, Case Western Reserve University, Cleveland, OH, 44106, USA;5. Geriatric Research, Education and Clinical Center, Louis Stokes Cleveland Department of Veterans Affairs Medical Center, Cleveland, OH, 44106, USA;6. Department of Pathology, University Hospitals Cleveland Medical Center, Division of Clinical Microbiology, Cleveland, OH, 44106, USA;7. University of North Carolina School of Medicine, Chapel Hill, NC, 27514, USA;8. Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, NJ, 07601, USA;9. Departments of Pharmacology, Molecular Biology & Microbiology, And Proteomics & Bioinformatics, Case Western Reserve University, Cleveland, OH, 44106, USA;10. CWRU-Cleveland VAMC Center for Antimicrobial Resistance and Epidemiology (Case VA CARES), Cleveland, OH, 44106, USA |
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| Abstract: | The synthesis of [4.3.0] fused pyrazolidinones is described. The compounds were prepared with substituents identical to those of the known antibacterial agents in the [3.3.0] pyrazolidinone series. Their preparation involved a six-membered ring annulation to a known pyrazolidinone monocycle. Appropriate deblocking and functionalization of the nuclei provided compounds suitable for biological evaluation. In contrast to their lower homologues, the [4.3.0] pyrazolidinones did not exhibit significant antibacterial activity. |
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