David J Wustrow
Affiliation: Neurogen Corporation
- Carboxylate bioisosteres of gabapentinCarmen 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...
- The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseasesLain 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...
- Aminopyrazine CB1 receptor inverse agonistsDavid 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...
- 1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonistsQin 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...
- 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 inflammationDaniel 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...
- Carboxylate bioisosteres of pregabalinJacob 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...
- 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 activityBastiaan 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...
- Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta proteinThomas 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...
- Heteroaromatic side-chain analogs of pregabalinRobert 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...