Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
A novel series of conformationally-restricted oxazolidinones was synthesized which possess a fused pyrazole ring substituted with various alkyl, aryl and heteroaryl substituents. A number of analogs exhibited potent activity against both gram-positive and fastidious gram-negative organisms.
Boyer
Frederick E
FE
Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. FDBoyer@sbcglobal.net
Vara Prasad
J V N
JV
Choy
Allison L
AL
Chupak
Louis
L
Dermyer
Michael R
MR
Ding
Qizhu
Q
Huband
Michael D
MD
Jiao
Wenhua
W
Kaneko
Takushi
T
Khlebnikov
Vladimir
V
Kim
Ji-Young
JY
Lall
Manjinder S
MS
Maiti
Samarendra N
SN
Romero
Karina
K
Wu
Xiujuan
X
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D015394:Molecular Structure; D023303:Oxazolidinones / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011720:Pyrazoles