Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones
Abstract
Conformationally constrained tetracyclic fluoroquinolones (FQs) were synthesized and profiled for their microbiological spectrum. The installation of a seven‐membered ring between the pyrrolidine substituents and the C8 position on the FQ core scaffold resulted in a remarkable enhancement of microbiological potency toward both Gram‐positive and Gram‐negative bacteria. Focused optimization of seven‐membered ring composition, stereochemistry, and amine placement led to the discovery of the two lead compounds that were selected for further progression.
Document Details
- Document Type
- Pub Defense Publication
- Publication Date
- Oct 02, 2017
- Source ID
- 10.1002/cmdc.201700426
Entities
People
- Adam A. Goldblum
- Allan S. Wagman
- Christina R. Harris
- George Miller
- Glenn Mcenroe
- Heinz E Moser
- James Aggen
- Lloyd J. Simons
- Marcela Gomez
- Martin S. Linsell
- Michael J. Melnick
- Ricky D. Gaston
- Ryan Cirz
- Sara Lopez
- Thomas R. Belliotti
- Toni‐jo Poel
Organizations
- Defense Threat Reduction Agency