New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
Exploration of the structure-activity relationships of the traditional C-5 acetamidomethyl side chain of the oxazolidonone antibacterials has yielded new, potent series of compounds of which the first examples, the O-linked iosoxazoles are described in detail, leading to the selection of the pre-clinical candidate AZD2563.
Gravestock
Michael B
MB
AstraZeneca R&D Boston, Infection Discovery, 35 Gatehouse Park, Waltham, MA 02451, USA. gravestock@astrazeneca.com
Acton
David G
DG
Betts
Michael J
MJ
Dennis
Michael
M
Hatter
Glenn
G
McGregor
Alexandra
A
Swain
Michael L
ML
Wilson
R Geoffrey
RG
Woods
Lisa
L
Wookey
Alan
A
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006838:Hydrocarbons; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry*; D051379:Mice; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013203:Staphylococcal Infections / Q000188:drug therapy*; D013211:Staphylococcus aureus / Q000472:pathogenicity; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; D006838:Hydrocarbons; D023303:Oxazolidinones; C030011:carbene; C453362:posizolid; D008697:Methane