Literature DB >> 15863314

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine.

Mark P Wentland1, Xufeng Sun, Yigong Bu, Rongliang Lou, Dana J Cohen, Jean M Bidlack.   

Abstract

8-Position variants of cyclazocine have been made where the phenolic 8-OH was replaced by thioamide, amidine, guanidine, urea and thiourea groups. High affinity for opioid receptors was observed for the 8-CSNH2 and 8-NHCHS analogues indicating that these groups are isosteric with not only the 8-OH but with the previously synthesized 8-CONH2 and 8-NHCHO cyclazocine derivatives.

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Year:  2005        PMID: 15863314     DOI: 10.1016/j.bmcl.2005.03.056

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  High-affinity carbamate analogues of morphinan at opioid receptors.

Authors:  Xuemei Peng; Brian I Knapp; Jean M Bidlack; John L Neumeyer
Journal:  Bioorg Med Chem Lett       Date:  2007-01-17       Impact factor: 2.823

2.  In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.

Authors:  Xuemei Peng; Brian I Knapp; Jean M Bidlack; John L Neumeyer
Journal:  Bioorg Med Chem       Date:  2007-03-30       Impact factor: 3.641

3.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.

Authors:  Mark P Wentland; Xufeng Sun; Dana J Cohen; Jean M Bidlack
Journal:  Bioorg Med Chem       Date:  2008-03-30       Impact factor: 3.641

4.  Use of Remifentanil in a Novel Clinical Paradigm to Characterize Onset and Duration of Opioid Blockade by Samidorphan, a Potent μ-Receptor Antagonist.

Authors:  Megan J Shram; Bernard Silverman; Elliot Ehrich; Edward M Sellers; Ryan Turncliff
Journal:  J Clin Psychopharmacol       Date:  2015-06       Impact factor: 3.153

5.  Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age.

Authors:  Vipul Kumar; Hong Lu; Marjie Hard; Lisa von Moltke
Journal:  Drugs R D       Date:  2019-09
  5 in total

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