Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds was written by Riether, Doris;Zindell, Renee;Wu, Lifen;Betageri, Raj;Jenkins, James E.;Khor, Someina;Berry, Angela K.;Hickey, Eugene R.;Ermann, Monika;Albrecht, Claudia;Ceci, Angelo;Gemkow, Mark J.;Nagaraja, Nelamangala V.;Romig, Helmut;Sauer, Achim;Thomson, David S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Electric Literature of C6H3FN2 This article mentions the following:
Through a ligand-based pharmacophore model (S)-proline based compounds were identified as potent cannabinoid receptor 2 (CB2) agonists with high selectivity over the cannabinoid receptor 1 (CB1). Structure-activity relationship investigations for this compound class lead to oxo-proline compounds I and II which combine an impressive CB1 selectivity profile with good pharmacokinetic properties. In a streptozotocin induced diabetic neuropathy model, II demonstrated a dose-dependent reversal of mech. hyperalgesia. In the experiment, the researchers used many compounds, for example, 6-Fluoronicotinonitrile (cas: 3939-12-6Electric Literature of C6H3FN2).
6-Fluoronicotinonitrile (cas: 3939-12-6) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Halopyridines are particularly attractive synthetic building blocks in a variety of cross-coupling methods, including the Suzuki-Miyaura cross-coupling reaction.Electric Literature of C6H3FN2