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

Jerzy Kossakowski; Marta Struga; Anna E Kozioł

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

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

Authors

Jerzy Kossakowski¹, Marta Struga, Anna E Kozioł

Affiliation

¹ The Medical University, Department of Medical Chemistry, 3 Oczki Str., 02-007 Warsaw.

PMID: 17203860

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.

MeSH terms

Adrenergic beta-Antagonists / chemical synthesis*
Adrenergic beta-Antagonists / metabolism
Adrenergic beta-Antagonists / pharmacology*
Animals
Cerebral Cortex / drug effects
Cerebral Cortex / metabolism
In Vitro Techniques
Indicators and Reagents
Ligands
Magnetic Resonance Spectroscopy
Models, Molecular
Piperazines / chemical synthesis*
Piperazines / pharmacology*
Propanols / chemical synthesis*
Propanols / pharmacology*
Propranolol / metabolism
Radioligand Assay
Rats
Triazoles / chemical synthesis*
Triazoles / pharmacology*

Substances

Adrenergic beta-Antagonists
Indicators and Reagents
Ligands
Piperazines
Propanols
Triazoles
Propranolol