title: Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
abstract: 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.
authors.affiliation: Discovery Research, Dr. Reddy's Laboratories Ltd, Miyapur, Hyderabad 500049, India. takhi@drreddys.com
authors.forename: Mohamed
authors.initials: M
authors.lastname: Takhi
authors.forename: Gurpreet
authors.initials: G
authors.lastname: Singh
authors.forename: C
authors.initials: C
authors.lastname: Murugan
authors.forename: Nirvesh
authors.initials: N
authors.lastname: Thaplyyal
authors.forename: Soma
authors.initials: S
authors.lastname: Maitra
authors.forename: K M
authors.initials: KM
authors.lastname: Bhaskarreddy
authors.forename: P V S
authors.initials: PV
authors.lastname: Amarnath
authors.forename: Arundhuti
authors.initials: A
authors.lastname: Mallik
authors.forename: T
authors.initials: T
authors.lastname: Harisudan
authors.forename: Ravi Kumar
authors.initials: RK
authors.lastname: Trivedi
authors.forename: K
authors.initials: K
authors.lastname: Sreenivas
authors.forename: N
authors.initials: N
authors.lastname: Selvakumar
authors.forename: Javed
authors.initials: J
authors.lastname: Iqbal