452092-31-8Relevant articles and documents
Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones
Wagman, Allan S.,Cirz, Ryan,McEnroe, Glenn,Aggen, James,Linsell, Martin S.,Goldblum, Adam A.,Lopez, Sara,Gomez, Marcela,Miller, George,Simons, Lloyd J.,Belliotti, Thomas R.,Harris, Christina R.,Poel, Toni-Jo,Melnick, Michael J.,Gaston, Ricky D.,Moser, Heinz E.
, p. 1687 - 1692 (2017/10/09)
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.
5-HYDROXYMETHYL-OXAZOLIDIN-2-ONE ANTIBACTERIALS
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Page/Page column 38, (2008/12/05)
The invention relates to novel chimeric antibiotics of formula (I) wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen
NOVEL ANTIBACTERIAL COMPOUNDS
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Page/Page column 55, (2010/11/25)
The invention relates to novel chimeric antibiotics of formula (I) Wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).