21653-99-6Relevant academic research and scientific papers
Using Small-Molecule Adjuvants to Repurpose Azithromycin for Use against Pseudomonas aeruginosa
Hubble, Veronica B.,Hubbard, Brittany A.,Minrovic, Bradley M.,Melander, Roberta J.,Melander, Christian
, p. 141 - 151 (2019)
A major contributor to fatalities in cystic fibrosis (CF) patients stems from infection with opportunistic bacterium Pseudomonas aeruginosa. As a result of the CF patient's vulnerability to bacterial infections, one of the main treatment focuses is antibiotic therapy. However, the highly adaptive nature of P. aeruginosa, in addition to the intrinsic resistance to many antibiotics exhibited by most Gram-negative bacteria, means that multi-drug-resistant (MDR) strains are increasingly prevalent. This makes the eradication of pseudomonal lung infections nearly impossible once the infection becomes chronic. New methods to treat pseudomonal infections are greatly needed in order to eradicate MDR bacteria found within the respiratory tract, and ultimately better the quality of life for CF patients. Herein, we describe a novel approach to combatting pseudomonal infections through the use of bis-2-aminoimidazole adjuvants that can potentiate the activity of a macrolide antibiotic commonly prescribed to CF patients as an anti-inflammatory agent. Our lead bis-2-AI exhibits a 1024-fold reduction in the minimum inhibitory concentration of azithromycin in vitro and displays activity in a Galleria mellonella model of infection.
Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers
Furlani, Robert E.,Richardson, Mike A.,Podell, Brendan K.,Ackart, David F.,Haugen, Jessica D.,Melander, Roberta J.,Basaraba, Randall J.,Melander, Christian
supporting information, p. 4820 - 4823 (2015/10/28)
The formation of advanced glycation end-products (AGE) as a result of the action of reducing sugars on host macromolecules plays a role in increased morbidity of diabetic patients. There are currently no clinically available therapeutics for the preventio
Synthesis and antinociceptive activity of some novel nonpeptide derivatives of interleukin-1β (193-195) sequence
Fantetti, Lia,Adembri, Giorgio,Giotti, Alberto,Masini, Ilaria,Roncucci, Gabrio
, p. 137 - 143 (2007/10/03)
The synthesis of a new series of nonpeptide derivatives of interleukin- 1β sequence is described. Compounds have been investigated for their relative activity regarding antinociception and suppression of inflammation. Several compounds with R1(
