49802-71-3Relevant articles and documents
Discovery of new C3aR ligands. Part 2: Amino-piperidine derivatives
Denonne, Frederic,Binet, Sophie,Burton, Maggi,Collart, Philippe,Defays, Sabine,Dipesa, Alan,Eckert, Maria,Giannaras, Alexander,Kumar, Seema,Levine, Beth,Nicolas, Jean-Marie,Pasau, Patrick,Pegurier, Cecile,Preda, Dorin,Van houtvin, Nathalie,Volosov, Andrew,Zou, Dong
, p. 3262 - 3265 (2008/02/08)
The synthesis and structure-activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.
Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators
Charton, Julie,Girault-Mizzi, Sophie,Debreu-Fontaine, Marie-Ange,Foufelle, Fabienne,Hainault, Isabelle,Bizot-Espiard, Jean-Guy,Caignard, Daniel-Henri,Sergheraert, Christian
, p. 4490 - 4518 (2007/10/03)
Design, synthesis and structure-activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. AMPK is the central component of a protein kinase cascade that plays a key role in the regulation of energy balance. Once activated, AMPK initiates a series of responses that are aimed at restoring the energy balance of the cell and recent studies have indicated that AMPK plays an important role in regulation of the whole-body energy metabolism. The following study based on the lead compound S27847 involved modification of three regions of this compound. Preliminary structure-activity relationships are being described.
Pharmacological studies and synthesis of morpholino alkyl derivatives
Saturnino, Carmela,Capasso, Anna,Lancelot, Jean-Chanles,Rault, Sylvain,Buonerba, Mariafrancesca,De Martino, Giovanni
, p. 1151 - 1154 (2007/10/03)
Seven morpholin derivatives were synthesized (compounds 1-7) and their behavioural effects were evaluated; the elements considered were locomotor activity, motor coordination, catalepsy, stereotyped behaviour and antinociception. All the compounds, at doses of 10-20-40 mg/kg/i.p., induced a reduction of all behavioural elements without a significant antinociceptive effect. These results indicate that these morpholin derivatives affect the central nervous system.