55746-20-8Relevant academic research and scientific papers
Oxygen-containing benzo-cycloaliphatic amine compounds
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, (2018/06/16)
The invention provides an oxygen-containing benzo-cycloaliphatic substituted amine compounds and application thereof and specifically relates to the oxygen-containing benzo-cycloaliphatic substitutedamine compounds as shown in a formula I which is described in the specification or pharmaceutically acceptable salts thereof and application of the same to preparation of Staphylococcus aureus goldenpigment synthesis inhibitor type antibacterial agents.
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model
Takahashi, Bitoku,Funami, Hideaki,Iwaki, Takehiko,Maruoka, Hiroshi,Shibata, Makoto,Koyama, Makoto,Nagahira, Asako,Kamiide, Yoshiyuki,Kanki, Satomi,Igawa, Yoshiyuki,Muto, Tsuyoshi
, p. 4792 - 4803 (2015/08/03)
A series of 2-alkylamino nicotinamide analogs was prepared as orally active ghrelin receptor (ghrelinR) inverse agonists. Starting from compound 1, oral bioavailability was improved by modifying metabolically unstable sites and reducing molecular weight. Brain-permeable compound 33 and compound 24 with low brain permeability were tested in rat models of obesity; 30 mg/kg of compound 33 suppressed weight gain. PK/PD analysis revealed that the anti-obesity effect of ghrelinR inverse agonists depends on their brain concentrations.
