119736-19-5Relevant academic research and scientific papers
Pyridone-conjugated monobactam antibiotics with gram-negative activity
Brown, Matthew F.,Mitton-Fry, Mark J.,Arcari, Joel T.,Barham, Rose,Casavant, Jeffrey,Gerstenberger, Brian S.,Han, Seungil,Hardink, Joel R.,Harris, Thomas M.,Hoang, Thuy,Huband, Michael D.,Lall, Manjinder S.,Lemmon, M. Megan,Li, Chao,Lin, Jian,McCurdy, Sandra P.,McElroy, Eric,McPherson, Craig,Marr, Eric S.,Mueller, John P.,Mullins, Lisa,Nikitenko, Antonia A.,Noe, Mark C.,Penzien, Joseph,Plummer, Mark S.,Schuff, Brandon P.,Shanmugasundaram, Veerabahu,Starr, Jeremy T.,Sun, Jianmin,Tomaras, Andrew,Young, Jennifer A.,Zaniewski, Richard P.
, p. 5541 - 5552 (2013/07/26)
Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity against clinically relevant Gram-negative species including Pseudomonas aeruginosa, Klebsiella pneumoniae, and Escherichia coli. Rat pharmacokinetic studies with compound 17 demonstrate low clearance and low plasma protein binding. In addition, evidence is provided for a number of analogues suggesting that the siderophore receptors PiuA and PirA play a role in drug uptake in P. aeruginosa strain PAO1.
Fluorinated derivatives of deferiprone
-
Page/Page column 28, (2008/12/07)
The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.
Antibiotic sulfonylaminocarbonyl activated beta-lactams
-
, (2008/06/13)
This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula STR1 wherein R401 and R402 are the same or different and are (a) hydrogen, (b) (C1 -C12) alkyl (c) (C2 -C8) alkenyl, (d) (C2 -C8) alkynyl, (e) (C3 -C10) cycloalkyl, (f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1 -C4) alkyl, and (C1 -C4) alkoxy, (h) --CH2 --O--CO--CH2 --NHR420, (i) --CH2 --O--CO2 --R430, (j) --CH2 F, or (k) --CHF2 ; wherein R420 is (a) hydrogen, (b) --COH, or (c) --CO--O--C(CH3)3 ; wherein R430 is (C1 -C8) alkyl, --(CH2) 2 OC(O)NH2, --(CH 2)2 Cl, --(CH2)2 OCH3 or --(CH2)2 NHCOH; wherein R300 is an acyl group derived from a carboxylic acid; wherein R100 is an optionally substituted heterocyclic moiety of Formula 2, 3, 4 or 5 STR2
