30067-11-9Relevant articles and documents
HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE
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Page/Page column 182, (2009/10/22)
The present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.
Design and biological evaluation of phenyl-substituted analogs of β-phenylethylidenehydrazine
Sowa, Bernard,Rauw, Gillian,Davood, Asghar,Fassihi, Afshin,Knaus, Edward E.,Baker, Glen B.
, p. 4389 - 4395 (2007/10/03)
β-Phenylethylidenehydrazine (PEH) has been demonstrated previously to be an inhibitor of γ-aminobutyric acid transaminase (GABA-T) and to cause a marked increase in rat brain levels of GABA, a major neurotransmitter. A group of PEH analogs, possessing a variety of substituents (Me, OMe, Cl, F, and CF3) at the 2-, 3-, and 4-positions of the phenyl ring, were synthesized for evaluation as inhibitors of GABA-T. The details of the synthesis and chemical characterization of the analogs are described. Preliminary in vitro screening for GABA-T inhibition showed that all the analogs possessed activity against this enzyme, although substitution of CF3 at the 2- and 4-positions caused reduced activity. One of the drugs, 4-fluoro-β- phenylethylidenehydrazine, was investigated further ex vivo, where it was shown to inhibit GABA-T, elevate brain levels of GABA, and decrease levels of glutamine, similar to the profile observed previously for PEH.