Pinard Emmanuel, Alberati Daniela, Alvarez-Sanchez Ruben, Brom Virginie, Burner Serge, Fischer Holger, Hauser Nicole, Kolczewski Sabine, Lengyel Judith, Mory Roland, Saladin Christian, Schulz-Gasch Tanja, Stalder Henri
Pharmaceutical Research Basel, F. Hoffmann-La Roche Ltd. , CH-4070 Basel, Switzerland.
ACS Med Chem Lett. 2014 Feb 4;5(4):428-33. doi: 10.1021/ml500005m. eCollection 2014 Apr 10.
3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration.
3-氨基-3-芳基哌啶被发现是一类新型的甘氨酸转运体1(GlyT1)抑制剂。所建立的构效关系使得能够鉴定出对甘氨酸转运体2(GlyT2)亚型具有优异选择性、具备类药物性质且口服给药后具有体内活性的高效化合物。