Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABAA antagonists: synthesis, pharmacology, and molecular modeling

…, C Sanchez, P Krogsgaard-Larsen…

Index: Froelund, Bente; Kristiansen, Uffe; Brehm, Lotte; Hansen, Annette B.; Krogsgaard-Larsen, Povl; Falch, Erik Journal of Medicinal Chemistry, 1995 , vol. 38, # 17 p. 3287 - 3296

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Citation Number: 55

Abstract

A number of analogues of the low-efficacy partial GABAA agonist 5-(4-piperidyl)-3- isoxazolol (4-PIOL, 5), in which the 4-position of the 3-isoxazolol ring was substituted by different groups, were synthesized and tested as GABAA receptor ligands. Substituents of different size and structural flexibility such as alkyl, phenylalkyl, diphenylalkyl, and naphthylalkyl were explored. Pharmacological characterization of the synthesized ...