A new series of tricyclic (aryloximino)propanolamines displaying very high selective beta 2-blocking properties.
A new class of indanones 4 easily obtained by aryne type condensations, followed by transposition of the benzocyclobutanols 3 thus formed, were transformed into the corresponding oximinopropanolamines 7. These compounds were studied for their potential beta-blocking properties. It was found that 7 have generally low beta 1-blocking properties. Their beta 2-blocking action varies from low to very high. Interestingly one of them (7b) has the highest beta 2 activity/beta 1 activity (343) value known to date.
Jamart-Gregoire
B
B
Laboratoire de Chimie Organique I, UA CNRS 457, Université de Nancy I, Vandoeuvre les Nancy, France.
Caubere
P
P
Blanc
M
M
Gnassounou
J P
JP
Advenier
C
C
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines