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.
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.
Kossakowski
Jerzy
J
The Medical University, Department of Medical Chemistry, 3 Oczki Str., 02-007 Warsaw.
Struga
Marta
M
Kozioł
Anna E
AE
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D020005:Propanols / Q000138:chemical synthesis* / Q000494:pharmacology*; D011433:Propranolol / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000319:Adrenergic beta-Antagonists; D007202:Indicators and Reagents; D008024:Ligands; D010879:Piperazines; D020005:Propanols; D014230:Triazoles; D011433:Propranolol