David J Wustrow

Summary

Affiliation: Neurogen Corporation
Country: USA

Publications

  1. ncbi request reprint Carboxylate bioisosteres of gabapentin
    Carmen E Burgos-Lepley
    Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 16:2333-6. 2006
  2. ncbi request reprint The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases
    Lain Yen Hu
    Pfizer Global Research and Development, Ann Arbor, MI, USA
    Bioorg Med Chem Lett 16:2337-40. 2006
  3. doi request reprint Aminopyrazine CB1 receptor inverse agonists
    David J Wustrow
    Neurogen Corporation, 35 Northeast Industrial Road, Branford CT 06405, USA
    Bioorg Med Chem Lett 18:3376-81. 2008
  4. doi request reprint 1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists
    Qin Guo
    Neurogen Corporation, 35 NE Industrial Road, Branford, CT 06405, USA
    Bioorg Med Chem Lett 18:5027-31. 2008
  5. doi request reprint Characterization of N-(adamantan-1-ylmethyl)-5-[(3R-amino-pyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 antagonist in animal models of pain and inflammation
    Daniel C Broom
    Department of Pharmacology, Neurogen Corporation, Branford, Connecticut, USA
    J Pharmacol Exp Ther 327:620-33. 2008
  6. ncbi request reprint Carboxylate bioisosteres of pregabalin
    Jacob B Schwarz
    Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, 48105, USA
    Bioorg Med Chem Lett 16:3559-63. 2006
  7. ncbi request reprint Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity
    Bastiaan J Venhuis
    Department of Medicinal Chemistry, University Centre for Pharmacy, University of Groningen, Antonius Deusinglaan 1, NL 9713 AV Groningen, The Netherlands
    J Med Chem 46:584-90. 2003
  8. ncbi request reprint Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein
    Thomas R Belliotti
    Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor Campus, Ann Arbor, MI, 48105, USA
    J Med Chem 48:2294-307. 2005
  9. ncbi request reprint Heteroaromatic side-chain analogs of pregabalin
    Robert M Schelkun
    PGRD Michigan Laboratories, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 16:2329-32. 2006

Collaborators

  • He Zhao
  • James E Krause
  • Kevin J Hodgetts
  • Synthia H Sun
  • David J Matson
  • Lain Yen Hu
  • Jacob B Schwarz
  • Mark G Vartanian
  • Qin Guo
  • Daniel C Broom
  • Robert M Schelkun
  • Carmen E Burgos-Lepley
  • Charles P Taylor
  • Thomas Capiris
  • Mark J Field
  • Jack J Kinsora
  • Thomas R Belliotti
  • Lawrence D Wise
  • Thomas G Heffner
  • Leonard T Meltzer
  • Bastiaan J Venhuis
  • Mark T Kershaw
  • Weifeng Yu
  • David Ihle
  • Daniel Broom
  • Jayaraman Chandrasekhar
  • Dawn Alderman
  • Michele Matchett
  • Daniel N Cortright
  • Daniel Cortright
  • Robin Meade
  • Elizabeth Bradshaw
  • Ricardo Ochoa
  • Kristen K Ford
  • Susan Coombs
  • Bertrand L Chenard
  • Charles Cheng
  • Jun Yuan
  • Yao Peng
  • Alan Hutchison
  • Jean Simmermacher-Mayer
  • Marianne E Buck
  • Nirmala Suman-Chauhan
  • Cindy M Donovan
  • Lisa R Thompson
  • Jack Kinsora
  • Susan M Lotarski
  • Ti Zhi Su
  • Ayman El-Kattan
  • Justin S Bryans
  • David J Dooley
  • Karen Walters
  • Po Wai Yuen
  • Simon A Osborne
  • Madhu Cherukury
  • Clare O Kneen
  • Mark L Weber
  • Ti Zhi-Su
  • I Victor Ekhato
  • Andrew J Thorpe
  • Durk Dijkstra
  • Stephen J Johnson
  • Håkan V Wikström

Detail Information

Publications9

  1. ncbi request reprint Carboxylate bioisosteres of gabapentin
    Carmen E Burgos-Lepley
    Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 16:2333-6. 2006
    ..Further characterization of alpha2-delta binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1...
  2. ncbi request reprint The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases
    Lain Yen Hu
    Pfizer Global Research and Development, Ann Arbor, MI, USA
    Bioorg Med Chem Lett 16:2337-40. 2006
    ..SAR, pharmacology, and the crystal structure of hBCATc with inhibitor 2 are described...
  3. doi request reprint Aminopyrazine CB1 receptor inverse agonists
    David J Wustrow
    Neurogen Corporation, 35 Northeast Industrial Road, Branford CT 06405, USA
    Bioorg Med Chem Lett 18:3376-81. 2008
    ..Optimized compounds were demonstrated to be inverse agonists and compared in vivo with rimonabant for their ability to inhibit food intake, to occupy central CB1 receptors and to influence hormonal markers associated with obesity...
  4. doi request reprint 1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists
    Qin Guo
    Neurogen Corporation, 35 NE Industrial Road, Branford, CT 06405, USA
    Bioorg Med Chem Lett 18:5027-31. 2008
    ..A number of compounds, for example, 38g, with excellent affinity for the cynomolgus macaque and rat bradykinin B(1) receptor were discovered...
  5. doi request reprint Characterization of N-(adamantan-1-ylmethyl)-5-[(3R-amino-pyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 antagonist in animal models of pain and inflammation
    Daniel C Broom
    Department of Pharmacology, Neurogen Corporation, Branford, Connecticut, USA
    J Pharmacol Exp Ther 327:620-33. 2008
    ..Further study of P2X(7) antagonists both in preclinical and clinical studies will help elucidate the role of the P2X(7) receptor in pain and inflammatory mechanisms and may help identify potential clinical benefits of such molecules...
  6. ncbi request reprint Carboxylate bioisosteres of pregabalin
    Jacob B Schwarz
    Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, 48105, USA
    Bioorg Med Chem Lett 16:3559-63. 2006
    ..Two select compounds with potent affinity for alpha(2)-delta, 8a and 16a, were subsequently tested in vivo in an audiogenic seizure model and found to elicit protective effects...
  7. ncbi request reprint Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity
    Bastiaan J Venhuis
    Department of Medicinal Chemistry, University Centre for Pharmacy, University of Groningen, Antonius Deusinglaan 1, NL 9713 AV Groningen, The Netherlands
    J Med Chem 46:584-90. 2003
    ..It is speculated that such metabolites are alpha'-hydroxylated enones that may constitute the first step in the formation of the corresponding catechols...
  8. ncbi request reprint Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein
    Thomas R Belliotti
    Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor Campus, Ann Arbor, MI, 48105, USA
    J Med Chem 48:2294-307. 2005
    ..However, both interactions appear to play an important role in the in vivo profile of these compounds...
  9. ncbi request reprint Heteroaromatic side-chain analogs of pregabalin
    Robert M Schelkun
    PGRD Michigan Laboratories, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 16:2329-32. 2006
    ..A series of heteroaromatic analogs of pregabalin has been identified that possess anticonvulsant activity in the DBA/2 mouse model. The methods of synthesis and preliminary pharmacology are discussed herein...