European Journal of Medicinal Chemistry (2020)
Update date:2022-08-15
Topics: Metabotropic Glutamate Receptor-2 (mGluR2) Positive Allosteric Modulators (PAMs) Dihydropyrazino-Benzimidazole Derivatives Discovery
Szabó, Gy?rgy
Kolok, Sándor
Orgován, Zoltán
Vastag, Mónika
Béni, Zoltán
Kóti, János
Sághy, Katalin
Lévay, Gy?rgy I.
Greiner, István
Keser?, Gy?rgy M.
A scaffold hopping strategy converted the known 1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidine core (1 and 2) by cyclization to a fused [6 + 5+6] membered heterocyclic mGluR2 PAM scaffold. Pharmacophore guided structure?activity relationship (SAR) studies resulted in a series of potent and metabolically stable mGluR2 PAMs. A representative optimized compound (95) having the most balanced profile, demonstrated efficacy in the PCP-induced hyper-locomotion model in mice that revealed the new chemotype being a promising PAM lead targeting mGluR2 receptors and providing support for further translational studies.
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