Compound ID | 833

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RWJ-416457

Class: Oxazolidinone

Spectrum of activity: Gram-negative
Details of activity: Protein synthesis inhibitor. Effective against MRSA, MSSA, Enterococcus faecium and Enterococcus faecalis - superior activity to linezolid in vitro, and in a murine model against S. pneumoniae
Propensity to select resistant mutants: Yes (10E-9)
Description: Santoro C, Bush K and Abbanat D. Characterisation of in vitro resistance to RWJ-416457 and linezolid in S. aureus, E. faecium and E. faecalis. 46th-ICAAC-2006;211.
Institute where first reported: Johnson & Johnson Pharmaceutical
Year first mentioned: 2002
Highest developmental phase: Preclinical
Development status: Inactive
Reason Dropped: Demonstrated insufficient improvement over linezolid- (LS)
Chemical structure(s):
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Molecular weight: 373.38
Iso. SMILES: CC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(=C(C=C2)N3CC4=CN(N=C4C3)C)F
InChI Key: UCBHICFFJKDMMR-AWEZNQCLSA-N
Can. SMILES: CC(=O)NC[C@H]1CN(C2=CC=C(C(=C2)F)N3CC4=CN(C)N=C4C3)C(=O)O1
InChI: InChI=1S/C18H20FN5O3/c1-11(25)20-6-14-9-24(18(26)27-14)13-3-4-17(15(19)5-13)23-8-12-7-22(2)21-16(12)10-23/h3-5,7,14H,6,8-10H2,1-2H3,(H,20,25)/t14-/m0/s1
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/15984076
Citation: https://journals.asm.org/doi/10.1128/aac.01017-06?url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&rfr_dat=cr_pub++0pubmed

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