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J Med Chem ; 19(2): 202-8, 1976 Feb.
Article in English | MEDLINE | ID: mdl-1249799

ABSTRACT

Since the previously investigated bis(tetrahydroisoquinolines) 1 and bis(benzylamines) 2 may be classified as 1,omega-diaryl-1,omega-alkanediamines, it appeared worthwhile to examine this structural concept as a guideline for predicting significant fibrinolytic activity. The prototype bis compounds 7, 14, 15, and 29-31, which were synthesized for this purpose, incorporate such molecular modifications as replacement of the tetrahydroisoquinoline nuclei of series 1 with tetrahydrobenzazepine (7) and tetrahydropyridoindole (14-15) nuclei. The latter compounds, as well as 29-31 which possess features common to both series 1 and 2, showed good to moderate activity in the standard rat (ip) screen. Significant departures from the 1,omega-diaryl-1,omega-alkanediamine structural concept led to compounds (35 and 40) of weak to moderate activity.


Subject(s)
Amines/chemical synthesis , Benzylamines/chemical synthesis , Diamines/chemical synthesis , Fibrinolytic Agents/chemical synthesis , Isoquinolines/chemical synthesis , Animals , Benzylamines/pharmacology , Diamines/pharmacology , Fibrinolysis/drug effects , Isoquinolines/pharmacology , Rats , Structure-Activity Relationship
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