Synthesis of some N-substituted aminoalkanol derivatives of 5,8-dimethyl-3b,9-epoxy-3a,4,5,6,7,8,9,9a-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione and 6,7-dimethyl-4,9-epoxy-3a,4,5,8,9,9a-hexahydro-1H-benzo[f]isoindole-1,3(2H)-dione with an expected b-adrenolytic activity.
Pindolol and propranolol are used in the treatment of cardiovascular diseases, including hypotension or hypertension and antiarrythmic. Moreover, in the light of current 5-HT receptors classification it is known the mentioned drugs possess high 5-HT1A/5-HT1B affinity. It allows to establish two ways of researches. Department of Medicinal Chemistry of Medical University of Warsaw reports on synthesis of new compounds, analogues of Propranolol and Pindolol. A series of 5,8-dimethyl-3b,9-epoxy-3a,4,5,6,7,8,9,9a-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione and 6,7-dimethyl-4,9-epoxy-3a,4,5,8,9,9a-hexahydro-1H-benzo[f]isoindole-1,3(2H)-dione have been designed with oxygen bridged rings. This property provides pharmacological activity increasing and toxicity decreasing.
Kossakowski
Jerzy
J
Department of Medical Chemistry, The Medical University of Warsaw, 3 Oczki Str., 02-007 Warsaw, Poland.
Raszkiewicz
Aldona
A
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis*; D004852:Epoxy Compounds / Q000138:chemical synthesis*; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis*; D054833:Isoindoles; D009682:Magnetic Resonance Spectroscopy
C501453:5,8-dimethyl-3b,9-epoxy-3a,4,5,6,7,8,9,9a-octahydro-1H-benzo(e)isoindole-1,3(2H)-dione; C501452:6,7-dimethyl-4,9-epoxy-3a,4,5,8,9,9a-hexahydro-1H-benzo(f)isoindole-1,3(2H)-dione; D000319:Adrenergic beta-Antagonists; D004852:Epoxy Compounds; D007202:Indicators and Reagents; D007211:Indoles; D054833:Isoindoles