Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC=0.25-2 microg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC=2-4 microg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model.
Takhi
Mohamed
M
Discovery Research, Dr. Reddy's Laboratories Ltd, Miyapur, Hyderabad 500049, India. takhi@drreddys.com
Singh
Gurpreet
G
Murugan
C
C
Thaplyyal
Nirvesh
N
Maitra
Soma
S
Bhaskarreddy
K M
KM
Amarnath
P V S
PV
Mallik
Arundhuti
A
Harisudan
T
T
Trivedi
Ravi Kumar
RK
Sreenivas
K
K
Selvakumar
N
N
Iqbal
Javed
J