16790-49-1Relevant articles and documents
Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant Enterococcus
Kaur, Jatinder,Cao, Xufeng,Abutaleb, Nader S.,Elkashif, Ahmed,Graboski, Amanda L.,Krabill, Aaron D.,Abdelkhalek, Ahmed Hassan,An, Weiwei,Bhardwaj, Atul,Seleem, Mohamed N.,Flaherty, Daniel P.
, p. 9540 - 9562 (2020/10/19)
Vancomycin-resistant enterococci (VRE) are the second leading cause of hospital-acquired infections (HAIs) attributed to a drug-resistant bacterium in the United States, and resistance to the frontline treatments is well documented. To combat VRE, we have repurposed the FDA-approved carbonic anhydrase drug acetazolamide to design potent antienterococcal agents. Through structure-activity relationship optimization we have arrived at two leads possessing improved potency against clinical VRE strains from MIC = 2 μg/mL (acetazolamide) to MIC = 0.007 μg/mL (22) and 1 μg/mL (26). Physicochemical properties were modified to design leads that have either high oral bioavailability to treat systemic infections or low intestinal permeability to treat VRE infections in the gastrointestinal tract. Our data suggest the intracellular targets for the molecules are putative α-carbonic and γ-carbonic anhydrases, and homology modeling and molecular dynamics simulations were performed. Together, this study presents potential anti-VRE therapeutic options to provide alternatives for problematic VRE infections.
CARBONIC ANHYDRASE INHIBITORS AND ANTIBIOTICS AGAINST MULTIDRUG RESISTANT BACTERIA
-
Paragraph 0087; 0089; 00101, (2020/07/14)
The invention described herein generally relates to novel therapeutic compounds, and in particular to carbonic anhydrase inhibitors as a narrow spectrum antibiotics against drug resistant bacteria and methods for treating those infection diseases in mammals using the described carbonic anhydrase inhibitors or a pharmaceutical formulation thereof.
Combination of two active substances
-
, (2008/06/13)
The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.