title: Design, synthesis and antimicrobial evaluation of novel 1,3-oxazolidin-2- one derivatives.
abstract: A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative) and in vitro antifungal activity against two pathogenic fungal strains namely, Candida albicans and Saccharomyces cerevisiae. All the synthesized compounds showed activity against Gram-positive bacteria. Compounds 12c and 12l exhibited maximum antibacterial activity against Gram-positive bacteria. However, against Gram-negative bacteria only five of screened compounds were found to be active. Compounds 12c and 12i displayed best antifungal activity against the tested fungi. Docking studies were carried out in order to gain insight into the mechanism of action and the binding mode of these compounds. These studies were in agreement with the biological data.
authors.affiliation: Department of Chemistry, National Institute of Technology, Kurukshetra-136119, India. chandna.nisha@gmail.com
authors.forename: Nisha
authors.initials: N
authors.lastname: Chandna
authors.forename: Jitander K
authors.initials: JK
authors.lastname: Kapoor
authors.forename: Varsha
authors.initials: V
authors.lastname: Goyal
authors.forename: Neeraj K
authors.initials: NK
authors.lastname: Aggarwal
authors.forename: Kotni Meena
authors.initials: KM
authors.lastname: Kumari
authors.forename: Manga
authors.initials: M
authors.lastname: Vijjulatha
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D023303:Oxazolidinones