Takrouri, Khuloud; Cooper, Harold D.; Spaulding, Adnrew; Zucchi, Paula; Koleva, Bilyana; Cleary, Dillon C.; Tear, Westley; Beuning, Penny J.; Hirsch, Elizabeth B.; Aggen, James B. published the artcile< Progress against Escherichia coli with the Oxazolidinone Class of Antibacterials: Test Case for a General Approach To Improving Whole-Cell Gram-Negative Activity>, COA of Formula: C6H5BrN2O2, the main research area is Escherichia oxazolidinone antibacterial gram neg permeation; Gram-negative; efflux pump; outer membrane permeability; oxazolidinones; porins.
Novel antibacterials with activity against the Gram-neg. bacteria associated with nosocomial infections, including Escherichia coli and other Enterobacteriaceae, are urgently needed due to the increasing prevalence of multidrug-resistant strains. A major obstacle that has stalled progress on nearly all small-mol. classes with potential for activity against these species has been achieving sufficient whole-cell activity, a difficult challenge due to the formidable outer membrane and efflux barriers intrinsic to these species. Using a set of compound design principles derived from available information relating physicochem. properties to Gram-neg. entry or activity, we synthesized and evaluated a focused library of oxazolidinone analogs, a currently narrow spectrum class of antibacterials active only against Gram-pos. bacteria. In this series, we have explored the effectiveness for improving Gram-neg. activity by identifying and combining beneficial structural modifications in the C-ring region. We have found polar and/or charge-carrying modifications that, when combined in hybrid C-ring analogs, appear to largely overcome the efflux and/or permeability barriers, resulting in improved Gram-neg. activity. In particular, those analogs least effected by efflux and the permeation barrier had significant zwitterionic character.
ACS Infectious Diseases published new progress about Antibiotics. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, COA of Formula: C6H5BrN2O2.