Literature DB >> 6796685

N-(Methanesulfonyl)-16-phenoxyprostaglandincarboxamides: tissue-selective, uterine stimulants.

T K Schaaf, J S Bindra, J F Eggler, J J Plattner, A J Nelson, M R Johnson, J W Constantine, H J Hess, W Elger.   

Abstract

In an effort to develop tissue-selective prostaglandin analogues resistant to the metabolic inactivating pathways of the natural materials, hybrid compounds modified both at C-1 with a sulfonimide moiety and in the n-amylcarbinol side chain with substituted phenoxy groups were synthesized and evaluated in a variety of in vitro models. Several of these analogues exhibited potent, tissue-selective, uterine stimulant activity, a finding subsequently confirmed in clinical studies with one member of this series, N-(methanesulfonyl)-16-phenoxy-omega-tetranor-PGE2-carboxamide (CP-34089/ZK-57671, sulprostone).

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Year:  1981        PMID: 6796685     DOI: 10.1021/jm00143a018

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


  1 in total

1.  Discovery of Novel Seven-Membered Prostacyclin Analogues as Potent and Selective Prostaglandin FP and EP3 Dual Agonists.

Authors:  Isamu Sugimoto; Tohru Kambe; Tomotaka Okino; Tetsuo Obitsu; Nobukazu Ohta; Taihei Nishiyama; Akihiro Kinoshita; Taku Fujimoto; Hiromu Egashira; Shinsaku Yamane; Satoshi Shuto; Kousuke Tani; Toru Maruyama
Journal:  ACS Med Chem Lett       Date:  2016-12-13       Impact factor: 4.345

  1 in total

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