Fragment-Based Optimization of Dihydropyrazino-Benzimidazolones as Metabotropic Glutamate Receptor‑2 Positive Allosteric Modulators against Migraine

Our previous scaffold-hopping attempts resulted in dihydropyrazino-benzimidazoles as metabotropic glutamate receptor-2 (mGluR2) positive allosteric modulators (PAMs) with suboptimal drug-like profiles. Here, we report an alternative fragment-based optimization strategy applied on the new dihydropyra...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-06, Vol.64 (12), p.8607-8620
Hauptverfasser:	Szabó, György, Erdélyi, Péter, Kolok, Sándor, Vastag, Mónika, Halász, Attila S, Kis-Varga, Istvánné, Lévay, György I, Béni, Zoltán, Kóti, János, Greiner, István, Keserű, György M
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzimidazoles - chemical synthesis Benzimidazoles - pharmacokinetics Benzimidazoles - therapeutic use Excitatory Amino Acid Agonists - chemical synthesis Excitatory Amino Acid Agonists - pharmacokinetics Excitatory Amino Acid Agonists - therapeutic use Male Migraine Disorders - drug therapy Molecular Structure Proof of Concept Study Pyrazines - chemical synthesis Pyrazines - pharmacokinetics Pyrazines - therapeutic use Rats Rats, Wistar Receptors, Metabotropic Glutamate - agonists Structure-Activity Relationship
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