Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 2, Pages 192-197Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00449
Keywords
TAARI agonist; 2-aminooxazoline; SAR; schizophrenia
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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.
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