Literature DB >> 18417347

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

Mark P Wentland1, Xufeng Sun, Dana J Cohen, Jean M Bidlack.   

Abstract

A series of 7,8- and 8,9-fused pyrimidinone, aminopyrimidine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in opioid receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carboxamide of 8-CAC. In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified.

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Year:  2008        PMID： 18417347      PMCID： PMC2441872          DOI： 10.1016/j.bmc.2008.03.066

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  13 in total

1.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.

Authors:  Mark P Wentland; Melissa VanAlstine; Robert Kucejko; Rongliang Lou; Dana J Cohen; Amy L Parkhill; Jean M Bidlack
Journal:  J Med Chem       Date:  2006-09-07       Impact factor: 7.446

2.  Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.

Authors:  Mark P Wentland; Qun Lu; Rongliang Lou; Yigong Bu; Brian I Knapp; Jean M Bidlack
Journal:  Bioorg Med Chem Lett       Date:  2005-04-15       Impact factor: 2.823

Review 3.  Cyclazocine revisited.

Authors:  S Archer; S D Glick; J M Bidlack
Journal:  Neurochem Res       Date:  1996-11       Impact factor: 3.996

4.  Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

Authors:  Y Cheng; W H Prusoff
Journal:  Biochem Pharmacol       Date:  1973-12-01       Impact factor: 5.858

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

Authors:  Mark P Wentland; Xufeng Sun; Yigong Bu; Rongliang Lou; Dana J Cohen; Jean M Bidlack
Journal:  Bioorg Med Chem Lett       Date:  2005-05-16       Impact factor: 2.823

6.  8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.

Authors:  M P Wentland; R Lou; Y Ye; D J Cohen; G P Richardson; J M Bidlack
Journal:  Bioorg Med Chem Lett       Date:  2001-03-12       Impact factor: 2.823

7.  Hydrogen bond structural group constants.

Authors:  M H Abraham; J A Platts
Journal:  J Org Chem       Date:  2001-05-18       Impact factor: 4.354

8.  Synthesis and bioactivity of 4,10-dimethyl-pyridino[2,3-h]quinolin-2(1H)-one-9-carboxylic acid and its esters.

Authors:  Qian Zhang; Ying Chen; Yun Qing Zheng; Peng Xia; Yi Xia; Zheng Yu Yang; Kenneth F Bastow; Susan L Morris-Natschke; Kuo Hsiung Lee
Journal:  Bioorg Med Chem       Date:  2003-03-20       Impact factor: 3.641

9.  10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.

Authors:  Ao Zhang; Wennan Xiong; Jean M Bidlack; James E Hilbert; Brian I Knapp; Mark P Wentland; John L Neumeyer
Journal:  J Med Chem       Date:  2004-01-01       Impact factor: 7.446

10.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.

Authors:  Melissa A VanAlstine; Mark P Wentland; Dana J Cohen; Jean M Bidlack
Journal:  Bioorg Med Chem Lett       Date:  2007-09-29       Impact factor: 2.823
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  1 in total

1.  Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.

Authors:  Gianfranco Balboni; Stella Fiorini; Anna Baldisserotto; Claudio Trapella; Yusuke Sasaki; Akihiro Ambo; Ewa D Marczak; Lawrence H Lazarus; Severo Salvadori
Journal:  J Med Chem       Date:  2008-08-05       Impact factor: 7.446
  1 in total

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