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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>...
Fluorine can flow into the environment after leakage or spill accidents and these excessive amounts can cause adverse effects on terrestrial ecosystems. Using three media (filter paper, soil, and filt...
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 electronic properties and relatively small size of fluorine endow it with considerable versatility as a bioisostere and it has found application as a substitute for lone pairs of electrons, the hy...
A novel series of tubulin polymerization inhibitors, based on fluorinated derivatives of isocombretastatin A-4 was synthesized with the goal of evaluating the effect of these compounds on the prolifer...
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 ...
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...
Testing of a dual tuned proton/fluorine MRI radio frequency coil Images were collected from plastic fluorine phantoms taped to the upper thigh of health volunteers. This trial was ...
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.
A subclass of organophosphates that have a FLUORINE atom substituted for one of the OXYGEN atoms.
A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as flouride (FLUORIDES) to prevent dental caries.
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...