Title : Synthesis and beta-adrenergic antagonist activity of novel (3-oxazolinyl-1,4-dihydropyridyl) propanolamines.

Pub. Date : 1992 Jul

PMID : 1359908






4 Functional Relationships(s)
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1 Replacement of the naphthyloxy moiety of propranolol by a 1-[1-(4-n-butyl)-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyrid yl] group resulted in a significant decrease in cardiac beta 1-adrenergic antagonist activity which indicates that this group is not a suitable isostere for an aryloxy moiety. naphthyloxy UDP-GlcNAc:betaGal beta-1,3-N-acetylglucosaminyltransferase 2 Homo sapiens
2 Replacement of the naphthyloxy moiety of propranolol by a 1-[1-(4-n-butyl)-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyrid yl] group resulted in a significant decrease in cardiac beta 1-adrenergic antagonist activity which indicates that this group is not a suitable isostere for an aryloxy moiety. Propranolol UDP-GlcNAc:betaGal beta-1,3-N-acetylglucosaminyltransferase 2 Homo sapiens
3 Replacement of the naphthyloxy moiety of propranolol by a 1-[1-(4-n-butyl)-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyrid yl] group resulted in a significant decrease in cardiac beta 1-adrenergic antagonist activity which indicates that this group is not a suitable isostere for an aryloxy moiety. 1-[1-(4-n-butyl)-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyrid yl UDP-GlcNAc:betaGal beta-1,3-N-acetylglucosaminyltransferase 2 Homo sapiens
4 1-(1-[4-n-Butyl-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyridy l])-3- isopropylamino-2-propanol (10) showed a modest beta 2-adrenergic antagonist selectivity for trachea (beta 2/beta 1 = 3:1). 1-(1-[4-n-butyl-3-(4,4-dimethyloxazolin-2-yl)-1,4-dihydropyridy l])-3- isopropylamino-2-propanol UDP-GlcNAc:betaGal beta-1,3-N-acetylglucosaminyltransferase 2 Homo sapiens