1.
ACS Med Chem Lett
; 7(2): 192-7, 2016 Feb 11.
Article
in English
| MEDLINE
| ID: mdl-26985297
ABSTRACT
2-Aminooxazolines were discovered as a novel structural class of TAAR1 ligands. Starting from a known adrenergic compound 1, structural modifications were made to obtain highly potent and selective TAAR1 ligands such as 12 (RO5166017), 18 (RO5256390), 36 (RO5203648), and 48 (RO5263397). These compounds exhibit drug-like physicochemical properties, have good oral bioavailability, and display in vivo activity in a variety of animal models relevant for psychiatric diseases and addiction.
2.
Eur J Med Chem
; 44(7): 2787-95, 2009 Jul.
Article
in English
| MEDLINE
| ID: mdl-19200624
ABSTRACT
Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected compounds is discussed.