1027134-68-4Relevant academic research and scientific papers
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
Barbachyn, Michael R.,Hutchinson, Douglas K.,Brickner, Steven J.,Cynamon, Michael H.,Kilburn, James O.,et al.
, p. 680 - 685 (1996)
During the course of our investigations in the oxazolidinone antibacterial agent area, we have identified a subclass with especially potent in vitro activity against mycobacteria. The salient structural feature of these oxazolidinone analogues, 6 (U-10048
Spectroscopic identification of intermediates and final products of the chiral pool synthesis of sutezolid
Bocian, Wojciech,Cielecka-Piontek, Judyta,Lewandowska, Kornelia,Michalska, Katarzyna,Mizera, Miko?aj,Pa?ys, Barbara
, (2020)
Sutezolid is a new oxazolidinone derivative currently in clinical trials to determine its safety and efficacy towards highly drug-resistant tuberculosis. The aim of the study was the spectroscopic identification of selected key intermediate products of th
RETRACTED ARTICLE: Design, synthesis of novel oxazolidino-amides/sulfonamides conjugates and their impact on antibacterial activity
Bharath, Yarlagadda,Alugubelli, Gopi Reddy,Sreenivasulu, Reddymasu,Rao, Mandava. V. Basaveswara
, p. 457 - 468 (2018/02/09)
Abstract: In view of generating new compounds for future drug development, we have synthesized oxazolidinones library of aryl amides and aryl sulfonamide derivatives. These compounds were screened in vitro against panel of susceptible and resistant Gram-p
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry
Yan, Shanshan,Miller, Marvin J.,Wencewicz, Timothy A.,Moellmann, Ute
supporting information; experimental part, p. 1302 - 1305 (2010/06/15)
A series of novel oxazolidinone antibiotics having [2.2.1] and [2.2.2] bicyclic oxazine moieties at the C-5 side chain of the A-ring was synthesized by nitroso Diels-Alder reactions, from three linezolid analogs containing morpholine, piperazine and thiomorpholine, respectively, as the C-ring components. Subsequent N-O bond cleavage generated oxazolidinones with 4-amino cyclo-2-en-1-ol substituents. The in vitro antibacterial activities of these oxazolidinone analogs were evaluated.
Substituted oxazine and thiazine oxazolidinone antimicrobials
-
, (2008/06/13)
A compound of structural Formula I: STR1 or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO2, SNR10 or S(O)NR10 ; R is (a) hydrogen, (b) C1 -C8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C1 -C8 alkoxy, C1 -C8 acyloxy or --O--CH2 --Ph, (c) C3 -C6 cycloalkyl, (d) amino, (e) C1 -C8 alkylamino, (f) C1 -C8 dialkylamino or (g) C1 -C8 alkoxy; R1 is H, except when X is O then R1 can be H, CH3, CN, CO2 H, CO2 R or (CH2)m R11 (m is 1 or 2); R2 is independently H, F or Cl; R3 is H except when X is O and R1 is CH3 then R3 can be H or CH3 ; R10 is independently H, C1 -C4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C1 -C8 alkoxy, amino, C1 -C8 alkylamino, or C1 -C8 dialkylamino) or p-toluenesulfonyl; R11 is hydrogen, OH, OR, OCOR, NH2, NHCOR or N(R10)2 ; and n is 0, 1 or 2. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
