Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
A new class of oxazolidinone antibacterials incorporating oxygen-, nitrogen-, or sulfur-containing heterobicyclic C-rings is described. The in vitro potency and in vivo efficacy of these conformationally constrained oxazolidinone analogs are discussed.
Renslo
Adam R
AR
Pfizer Global Research and Development, 34790 Ardentech Ct., Fremont, CA 94555, USA.
Gao
Hongwu
H
Jaishankar
Priyadarshini
P
Venkatachalam
Revathy
R
Gómez
Marcela
M
Blais
Johanne
J
Huband
Michael
M
Vara Prasad
J V N
JV
Gordeev
Mikhail F
MF
D000577:Amides / Q000737:chemistry; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D051379:Mice; D008968:Molecular Conformation; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry*
D000577:Amides; D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D023303:Oxazolidinones; D013438:Sulfhydryl Compounds