title: Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
abstract: Novel oxazolidinones were synthesized containing a number of substituted five-membered heterocycles attached to the 'piperazinyl-phenyl-oxazolidinone' core of eperezolid. Further, the piperazine ring of the core was replaced by other diamino-heterocycles. These modifications led to several compounds with potent activity against a spectrum of resistant and susceptible gram-positive organisms, along with the identification of ranbezolid (RBx 7644) as a clinical candidate.
authors.affiliation: Department of Medicinal Chemistry, Ranbaxy Research Laboratory, Plot-20, Sector-18, Udyog Vihar, Gurgaon 122001, India. biswajit.das@ranbaxy.com
authors.forename: Biswajit
authors.initials: B
authors.lastname: Das
authors.forename: Sonali
authors.initials: S
authors.lastname: Rudra
authors.forename: Ajay
authors.initials: A
authors.lastname: Yadav
authors.forename: Abhijit
authors.initials: A
authors.lastname: Ray
authors.forename: A V S Raja
authors.initials: AV
authors.lastname: Rao
authors.forename: A S S V
authors.initials: AS
authors.lastname: Srinivas
authors.forename: Ajay
authors.initials: A
authors.lastname: Soni
authors.forename: Suman
authors.initials: S
authors.lastname: Saini
authors.forename: Shalini
authors.initials: S
authors.lastname: Shukla
authors.forename: Manisha
authors.initials: M
authors.lastname: Pandya
authors.forename: Pragya
authors.initials: P
authors.lastname: Bhateja
authors.forename: Sunita
authors.initials: S
authors.lastname: Malhotra
authors.forename: Tarun
authors.initials: T
authors.lastname: Mathur
authors.forename: S K
authors.initials: SK
authors.lastname: Arora
authors.forename: Ashok
authors.initials: A
authors.lastname: Rattan
authors.forename: Anita
authors.initials: A
authors.lastname: Mehta
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006571:Heterocyclic Compounds; D051379:Mice; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013203:Staphylococcal Infections / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D005663:Furans; D006571:Heterocyclic Compounds; D010080:Oxazoles; D023303:Oxazolidinones; C476340:ranbezolid