93107-14-3Relevant academic research and scientific papers
Anionic fluoroquinolones as antibacterials against biofilm-producing Pseudomonas aeruginosa
Long, Timothy E.,Keding, Lexie C.,Lewis, Demetria D.,Anstead, Michael I.,Withers, T. Ryan,Yu, Hongwei D.
, p. 1305 - 1309 (2016)
Pseudomonas aeruginosa is a common biofilm-forming bacterial pathogen implicated in diseases of the lungs. The extracellular polymeric substances (EPS) of respiratory Pseudomonas biofilms are largely comprised of anionic molecules such as rhamnolipids and
ANTIBIOTIC RESISTANCE BREAKERS
-
, (2019/01/05)
The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, -C(=NR')-NR'R'' or –CH2- CH=CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.
2-Aminoquinazolin-4(3H)-one as an Organocatalyst for the Synthesis of Tertiary Amines
Thakur, Maheshwar S.,Nayal, Onkar S.,Upadhyay, Rahul,Kumar, Neeraj,Maurya, Sushil K.
supporting information, p. 1359 - 1362 (2018/03/09)
The potential of 2-aminoquinazolin-4(3H)-one as an organocatalyst for the activation of aldehydes via noncovalent interaction for the synthesis of tertiary amines using formic acid as a reducing agent is reported for the first time. The developed protocol demonstrated a dilated substrate scope for aromatic and aliphatic amines with aromatic and aliphatic aldehydes. Furthermore, the current method was also fruitful for the derivatization of ciprofloxacin and its derivative in good to excellent yields.
Pharmacological characterization of 7-(4-(Piperazin-1-yl)) ciprofloxacin derivatives: Antibacterial activity, cellular accumulation, susceptibility to efflux transporters, and intracellular activity
Marquez, Beatrice,Pourcelle, Vincent,Vallet, Coralie M.,Mingeot-Leclercq, Marie-Paule,Tulkens, Paul M.,Marchand-Bruynaert, Jacqueline,Van Bambeke, Francoise
, p. 1290 - 1301 (2014/06/24)
Purpose: To evaluate pharmacological properties (antibacterial activity; accumulation in phagocytic cells; activity against intracellular bacteria; susceptibility to fluoroquinolone efflux transporters) of ciprofloxacin derivatives modified at C-7 of the
Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2
Tynebor, Robert M.,Chen, Meng-Hsin,Natarajan, Swaminathan R.,O'Neill, Edward A.,Thompson, James E.,Fitzgerald, Catherine E.,O'Keefe, Stephen J.,Doherty, James B.
, p. 5971 - 5975 (2012/11/07)
This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and 24 h coverage in the rat arthritis efficacy model.
