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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-doped VOsub>2</sub>(M) nanoparticles have been successfully synthesized using the hydrothermal method at a supercritical temperature of 490°C. The pristine VO<sub>2</sub>...
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 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...
The fluorination of the polymer polyethylene terephthalate in plasma created from SF₆ or CF₄ gas at various pressures was investigated. The surface was analysed by X-ray photoelectron spectroscopy...
MiR-132, miR-204 and BDNF-TrkB signaling pathway may be involved in spatial learning and memory impairment of the offspring rats caused by fluorine and aluminum exposure during the embryonic stage and into adulthood.
Fluorine and aluminium are nervous system poisons, but it remains unclear whether combined fluorine and aluminium exposure damages spatial learning and memory and, if so, by what mechanism. This study...
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...