Todd A Brugel

Summary

Affiliation: AstraZeneca R and D

Publications

  1. ncbi SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2
    Todd A Brugel
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:5405-10. 2010
  2. ncbi Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1
    Todd A Brugel
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:5847-52. 2010
  3. ncbi 4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators
    Hui Xiong
    CNS Discovery, AstraZeneca Pharmaceuticals, Wilmington, DE, USA
    Bioorg Med Chem Lett 20:7381-4. 2010
  4. ncbi Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1
    Jeffrey G Varnes
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:4878-81. 2010
  5. ncbi Identification of short-acting ?-opioid receptor antagonists with anxiolytic-like activity
    Matthew F Peters
    AstraZeneca Pharmaceuticals, Wilmington, DE 19850, United States
    Eur J Pharmacol 661:27-34. 2011

Collaborators

  • Dean G Brown
  • Matthew F Peters
  • Gaochao Tian
  • Philip D Edwards
  • Timothy M Piser
  • Jeffrey G Varnes
  • Hui Xiong
  • Francis M McLaren
  • Becky Brockel
  • Thomas R Simpson
  • Linda A Sygowski
  • Methvin Isaac
  • Reto A Gadient
  • John P McCauley
  • Gerard M Koether
  • Lindsay Hinkley
  • Kelly A Brush
  • Minli Zhang
  • Megan M King
  • James M Woods
  • Nathan Spear
  • Nathalie Breysse
  • Valerie Hoesch
  • Caprice Hightower
  • Vijay Chhajlani
  • Reed W Smith
  • Michael Balestra
  • Julie M Wilson
  • Abdelmalik Slassi
  • Jalaj Arora
  • James Kang
  • Laura M Panko

Detail Information

Publications5

  1. ncbi SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2
    Todd A Brugel
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:5405-10. 2010
    ..Changes to the linker conformation and identity as well as to the benzamide ring moiety were also investigated...
  2. ncbi Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1
    Todd A Brugel
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:5847-52. 2010
    ..2.1]octan-3-yloxy-benzamides showing potent and selectivity ? antagonism as well as good brain exposure. Analog 6c (? IC(50)=20 nM; ?:?=36, ?:?=415) was also shown to reverse ?-agonist induced rat diuresis in vivo...
  3. ncbi 4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators
    Hui Xiong
    CNS Discovery, AstraZeneca Pharmaceuticals, Wilmington, DE, USA
    Bioorg Med Chem Lett 20:7381-4. 2010
    ..Several analogs have excellent activity and desired drug-like properties. Compound 2b was further characterized as a PAM using several in vitro experiments, and produced robust activity in several preclinical animal models...
  4. ncbi Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1
    Jeffrey G Varnes
    CNS Discovery Research, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA
    Bioorg Med Chem Lett 20:4878-81. 2010
    ..Favorable brain-plasma ratios were observed for select compounds in pharmacokinetic studies to evaluate CNS penetration...
  5. ncbi Identification of short-acting ?-opioid receptor antagonists with anxiolytic-like activity
    Matthew F Peters
    AstraZeneca Pharmaceuticals, Wilmington, DE 19850, United States
    Eur J Pharmacol 661:27-34. 2011
    ..This further supports ?-opioid receptor as a promising target for developing novel psychiatric medications...