https://chemistry.mdma.ch/hiveboard/rhodium/pdf/archive/merbst/quinoline1999.pdf

Quinoline, quinazoline and acridone alkaloids

Gaba transporter heterogeneity: pharmacology and cellular localization

Recent Advances in the Friedländer Reaction

Diverse radiochemistry is an essential component of nuclear medicine; this includes imaging techniques such as positron emission tomography (PET). As such, PET can track diseases at an early stage of development, help patient care planning through personalized medicine and support drug discovery programs. Fluorine-18 is the most frequently used radioisotope in PET radiopharmaceuticals for both clinical and preclinical research. Its physical and nuclear characteristics (97% β+ decay, 109.8 min half-life, 635 keV positron energy) and high specific activity make it an attractive nuclide for labeling and molecular imaging. Arenes and heteroarenes are privileged candidates for 18F-incorporation as they are metabolically robust and therefore widely used by medicinal chemists and radiochemists alike. For many years, the range of (hetero)arenes amenable to 18F-fluorination was limited by the lack of chemically diverse precursors, and of radiochemical methods allowing 18F-incorporation in high selectivity and effi...

18F-Labeling of Arenes and Heteroarenes for Applications in Positron Emission Tomography

Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.

Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

/pdf/synthesis-of-fluorine-18-labeled-gaba-uptake-inhibitors-1c97eh3rhx.pdf

Synthesis of fluorine-18 labeled GABA uptake inhibitors

The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties

A lipophilic derivative of the known GABA uptake inhibitor guvacine has been prepared. The synthesis of this compound, [1-]2-bis 4-(trifluoromethyl)]phenyl[-methoxy]ethyl[- 1,2,5,6-tet-rahydro-3-pyridine carboxylic acid, monohydrochloride, Cl-966, is described. Studies were carried out to determine the metabolic profile of Cl-966, in rats. Two metabolites, one less polar and the other more polar than Cl-966, were identified and their structures assigned by spectroscopic methods and confirmed by comparison to synthetic material.

Vlad E. Gregor

Papers

Acetylcholinesterase inhibition by fused dihydroquinazoline compounds

Synthesis of fluorine-18 labeled GABA uptake inhibitors

The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties

Synthesis and metabolic profile of Cl‐966: A potent, orally‐active inhibitor of GABA uptake

Acetylcholinesterase Inhibition by Fused Dihydroquinazoline Compounds.