Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
Novel oxazolidinone antibacterials containing N-hydroxyacetamidine moiety are synthesized with the diversity at C-5 terminus. These compounds have been evaluated against a panel of clinically relevant gram-positive and gram-negative pathogens. Most of the analogs in this series displayed activity superior to Linezolid and in vivo efficacies of selected oxazolidinones are also disclosed herein.
Anti-infectives Group, Discovery Research, Dr. Reddy's Laboratoties Ltd, Miyapur Hyderabad 500-049, India. takhi@drreddys.com
Mohamed
M
Takhi
C
C
Murugan
M
M
Munikumar
K M
KM
Bhaskarreddy
Gurpreet
G
Singh
K
K
Sreenivas
M
M
Sitaramkumar
N
N
Selvakumar
J
J
Das
Sanjay
S
Trehan
Javed
J
Iqbal
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D006090:Gram-Negative Bacteria / Q000187:drug effects; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006877:Hydroxamic Acids / Q000737:chemistry*; D051379:Mice; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism
D000900:Anti-Bacterial Agents; D006877:Hydroxamic Acids; D023303:Oxazolidinones; C006358:acetohydroxamic acid