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Human African Trypanosomiasis, also known as African sleeping sickness, is caused by the parasitic protozoa of the genus Trypanosoma. If there is no pharmacological intervention, the parasites can cross the blood-brain barrier (BBB), inevitably leading to death of the patients. Previous investigation identified the quinolone amide GHQ168 as a promising lead compound having a nanomolar activity against T. b. brucei. Here, the role of a fluorine substitution at different positions was investigated in regard to toxicity, pharmacokinetics, and antitrypanosomal activity. This 'fluorine walk' led to new compounds with improved metabolic stability and consistent activity against T. b. brucei. The ability of the new quinolone amides to cross the BBB was confirmed using an F-labelled quinolone amide derivative by means of ex vivo autoradiography of a murine brain.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Fluorine has been recognized to selectively stabilize anatase titanium dioxide (TiO₂) crystal facets, however, resolving its physical location at the nanometer scale remains empirically elusive. Her...
Activation of carbon-fluorine (C-F) bonds is an important topic in synthetic organic chemistry recently. Among the methods for C-F bond cleavage, metal mediated and catalyzed β- or α-fluorine elimin...
The synthesis of chiral fluorine-containing motifs, especially chiral fluorine molecules with two contiguous stereogenic centers have been gaining current interest in research due to the limited numbe...
Fabrication of advanced electrocatalysts with high activity and durability is urgently needed to achieve energy conversion and pollution treatment at the same time. Herein, we highlight a fluorine-dop...
The ability of fluorine to serve as a hydrogen-bond acceptor has been debated for many years. Short fluorine-hydrogen contacts are thought to play a key role in stabilizing some complex supramolecular...
This pilot trial studies how well fluorine F 18 clofarabine positron emission tomography (PET)/computed tomography (CT) works in imaging patients with autoimmune or inflammatory diseases. ...
RATIONALE: Fluorine F 18 FEQA may be an effective radioactive drug to use with positron emission tomography (PET) scans. PURPOSE: This clinical trial is studying the use of fluorine F 18 ...
This trial studies how well fluorine F 18 fluorthanatrace positron emission tomography (PET)/computed tomography (CT) works in treating participants ovarian, fallopian tube, or primary per...
RATIONALE: Diagnostic procedures using fluorine F 18 EF5 and positron emission tomography to detect tumor hypoxia may help in planning cancer treatment. PURPOSE: This phase I trial is stu...
This phase II trial studies how well fluorine F 18 DCFPyL positron emission tomography/computed tomography (PET/CT) works in imaging participants with prostate cancer that has come back. D...
Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes.
Inorganic compounds that contain fluorine as an integral part of the molecule.
Magnetic resonance imaging diagnostic technique which uses fluorine-19 perfluorocarbon probes and contrast agents for high resolution image detection and quantitation.
Derivatives of BENZENE that contain FLUORINE.
A subclass of organophosphates that have a FLUORINE atom substituted for one of the OXYGEN atoms.
Tropical Medicine is the study of diseases more commonly found in tropical regions than elsewhere. Examples of these diseases are malaria, yellow fever, Chagas disease, Dengue, Helminths, African trypanosomiasis, Leishmaniasis, Leprosy, Lymphatic filaria...