Synthesis of GABAA receptor agonists and evaluation of their α-subunit selectivity and orientation in the GABA binding Site

M Jansen, H Rabe, A Strehle, S Dieler…

Index: Jansen, Michaela; Rabe, Holger; Strehle, Axelle; Dieler, Sandra; Debus, Fabian; Dannhardt, Gerd; Akabas, Myles H.; Lueddens, Hartmut Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4430 - 4448

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Citation Number: 27

Abstract

Drugs used to treat various disorders target GABAA receptors. To develop α subunit selective compounds, we synthesized 5-(4-piperidyl)-3-isoxazolol (4-PIOL) derivatives. The 3-isoxazolol moiety was substituted by 1, 3, 5-oxadiazol-2-one, 1, 3, 5-oxadiazol-2-thione, and substituted 1, 2, 4-triazol-3-ol heterocycles with modifications to the basic piperidine substituent as well as substituents without basic nitrogen. Compounds were screened by [ ...