Literature DB >> 6146718

[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.

S T Kam, W L Matier, K X Mai, C Barcelon-Yang, R J Borgman, J P O'Donnell, H F Stampfli, C Y Sum, W G Anderson, R J Gorczynski.   

Abstract

Novel [(arylcarbonyl)oxy]propanolamines were synthesized and investigated as potential ultrashort-acting beta-adrenergic receptor blockers. Many of these analogues exhibited good potency and short duration. The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog. It has been selected as a candidate for further clinical study. Structure-activity relationships and structure-duration relationships for these new beta-blockers are also discussed.

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Year:  1984        PMID: 6146718     DOI: 10.1021/jm00374a013

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Novel Type of Prodrug Activation through a Long-Range O,N-Acyl Transfer: A Case of Water-Soluble CREB Inhibitor.

Authors:  Bingbing X Li; Fuchun Xie; Qiuhua Fan; Kerry M Barnhart; Curtis E Moore; Arnold L Rheingold; Xiangshu Xiao
Journal:  ACS Med Chem Lett       Date:  2014-08-22       Impact factor: 4.345

2.  Modifying methoxycarbonyl etomidate inter-ester spacer optimizes in vitro metabolic stability and in vivo hypnotic potency and duration of action.

Authors:  S Shaukat Husain; Ervin Pejo; Rile Ge; Douglas E Raines
Journal:  Anesthesiology       Date:  2012-11       Impact factor: 7.892

  2 in total

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