Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
Design and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported. Their antibacterial activities have been evaluated in a MIC assay against broader panel of both susceptible and resistant Gram-positive strains. (S)-N-{3-[3-Fluoro-4-(methyl-{1-[3-(5-nitrofuran-2-yl)-acryloyl]-piperidin-4-yl}-amino)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 4i has shown comparable antibacterial activity to linezolid and eperezolid in the MIC assay, additionally compound 4i showed good antibacterial activity with an in vitro MIC value of 2-4 microg/mL against linezolid resistant Staphylococcus aureus (linezolid 16 microg/mL).
Srivastava
Brijesh Kumar
BK
Zydus Research Centre, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad 382210, India. brijeshsrivastava@zyduscadila.com
Soni
Rina
R
Patel
Jayendra Z
JZ
Solanki
Manish
M
Valani
Darshan
D
Gupta
Sunil
S
Mishra
Bhupendra
B
Takale
Vijay
V
Pandya
Purvi
P
Jain
Mukul R
MR
Patel
Pankaj R
PR
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010880:Piperidines