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具有预期β-肾上腺素能阻断活性的新型1-(氨基)-3-[(1,5-二苯基-1H-1,2,4-三唑-3-基)氧基]丙-2-醇和1-[(1,5-二苯基-1H-1,2,4-三唑-3-基)氧基]-3-(4-芳基哌嗪-1-基)丙-2-醇衍生物的合成

Synthesis of new 1-(amino)-3-[(1,5-diphenyl-1H-1,2,4-triazol-3-yl) oxy] propan-2-ol and 1-[(1,5-diphenyl- 1H- 1,2,4-triazol-3-yl) oxy]-3-(4-arylpiperazin-1-yl) propan-2-ol derivatives with an expected beta-adrenolytic activity.

作者信息

Kossakowski Jerzy, Struga Marta, Kozioł Anna E

机构信息

The Medical University, Department of Medical Chemistry, 3 Oczki Str., 02-007 Warsaw.

出版信息

Acta Pol Pharm. 2006 Jul-Aug;63(4):255-9.

Abstract

3-(Oxiran-2-ylmethoxy)-l ,5-diphenyl-lH-1,2,4-triazole [I] was obtained in the reaction of 1,5-di-phenyl-IH-1,2,4-triazol-3-ol with 2-(chloromethyl) oxirane. Then I was converted into the corresponding aminoalkanol derivatives of 1,5-diphenyl-IH-1,2,4-triazol-3-ol, IIa,b -VIIa,b. Molecular structure of I was confirmed by an X- ray structure analysis. The receptor affinities for IVa, VIIa were determined.

摘要

3-(环氧乙烷-2-基甲氧基)-1,5-二苯基-1H-1,2,4-三唑[I]是由1,5-二苯基-1H-1,2,4-三唑-3-醇与2-(氯甲基)环氧乙烷反应制得。然后将I转化为1,5-二苯基-1H-1,2,4-三唑-3-醇的相应氨基烷醇衍生物IIa,b - VIIa,b。通过X射线结构分析确定了I的分子结构。测定了IVa、VIIa的受体亲和力。

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