Synthesis and Biological Evaluation of 4-(Aminomethyl)-1-hydroxypyrazole Analogues of Muscimol as γ-Aminobutyric AcidA Receptor Agonists

…, J Kehler, K Frydenvang, J Kristensen…

文献索引：Petersen, Jette G.; Bergmann, Rikke; Moller, Henriette A.; Jorgensen, Charlotte G.; Nielsen, Birgitte; Kehler, Jan; Frydenvang, Karla; Kristensen, Jesper; Balle, Thomas; Jensen, Anders A.; Kristiansen, Uffe; Frolund, Bente Journal of Medicinal Chemistry, 2013 , vol. 56, # 3 p. 993 - 1006

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被引用次数: 11

摘要

A series of bioisosteric 4-(aminomethyl)-1-hydroxypyrazole (4-AHP) analogues of muscimol, a GABAA receptor agonist, has been synthesized and pharmacologically characterized at native and selected recombinant GABAA receptors. The unsubstituted 4-AHP analogue (2a)(EC50 19 μM, R max 69%) was a moderately potent agonist at human α1β2γ2 GABAA receptors, and in SAR studies substitutions in the 3-and/or 5-position were found to be ...