Sato, Nagaaki; Ando, Makoto; Ishikawa, Shiho; Jitsuoka, Makoto; Nagai, Keita; Takahashi, Hirobumi; Sakuraba, Aya; Tsuge, Hiroyasu; Kitazawa, Hidefumi; Iwaasa, Hisashi; Mashiko, Satoshi; Gomori, Akira; Moriya, Ryuichi; Fujino, Naoko; Ohe, Tomoyuki; Ishihara, Akane; Kanatani, Akio; Fukami, Takehiro published the artcile< Discovery of Tetrasubstituted Imidazolines as Potent and Selective Neuropeptide Y Y5 Receptor Antagonists: Reduced Human Ether-a-go-go Related Gene Potassium Channel Binding Affinity and Potent Antiobesity Effect>, COA of Formula: C6H11NO2, the main research area is aminoester fluorophenylmagnesium bromide bromofluoropyridine coupling ring opening closure reduction; imidazoline asym preparation; neuropeptide Y5 receptor antagonist antiobesity structure activity human.
A series of novel imidazoline derivatives was synthesized and evaluated as neuropeptide Y (NPY) Y5 receptor antagonists. Optimization of previously reported imidazoline leads, I and II, was attempted by introduction of substituents at the 5-position on the imidazoline ring and modification of the bis(4-fluorophenyl) moiety. A number of potent derivatives without human ether-a-go-go related gene potassium channel (hERG) activity were identified. Selected compounds, including III, were shown to have excellent brain and CSF permeability. Compound III displayed a suitable pharmacokinetic profile for chronic in vivo studies and potently inhibited D-Trp34NPY-induced acute food intake in rats. Oral administration of III resulted in a potent reduction of body weight in a diet-induced obese mouse model.
Journal of Medicinal Chemistry published new progress about Amino acid esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6136-93-2 belongs to class nitriles-buliding-blocks, and the molecular formula is C6H11NO2, COA of Formula: C6H11NO2.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts