Zhaoning Zhu

Summary

Affiliation: Schering-Plough Research Institute
Country: USA

Publications

  1. doi Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 51:725-36. 2008
  2. doi Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 19:5218-21. 2009
  3. doi Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 53:951-65. 2010
  4. doi The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease
    Hongmei Li
    Department of Medicinal Chemistry, Merck Research Laboratory, 126 E Lincoln Avenue, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 23:466-71. 2013
  5. doi Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation
    Mihirbaran Mandal
    Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States
    J Med Chem 55:9331-45. 2012
  6. doi Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor
    Jared N Cumming
    Merck Research Laboratories, 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 22:2444-9. 2012
  7. doi Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists
    Zhong Yue Sun
    Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 19:6801-5. 2009
  8. doi Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo
    Zhong Yue Sun
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States
    J Med Chem 55:489-502. 2012
  9. doi Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket
    Robert D Mazzola
    Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 18:5809-14. 2008
  10. ncbi Structure and activity relationships of tartrate-based TACE inhibitors
    Dansu Li
    Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, 320 Bent Street, Cambridge, MA 02141, United States
    Bioorg Med Chem Lett 20:4812-5. 2010

Collaborators

Detail Information

Publications14

  1. doi Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 51:725-36. 2008
    ..Mode A inhibitors occupy the S1'-S3' binding pockets, whereas mode B resides in the nonprime binding sites...
  2. doi Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 19:5218-21. 2009
    ..The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR development of the novel dopamine antagonists...
  3. doi Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation
    Zhaoning Zhu
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA
    J Med Chem 53:951-65. 2010
    ....
  4. doi The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease
    Hongmei Li
    Department of Medicinal Chemistry, Merck Research Laboratory, 126 E Lincoln Avenue, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 23:466-71. 2013
    ..These SAR explorations offer opportunities to identify potential drugs to treat Alzheimer's disease...
  5. doi Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation
    Mihirbaran Mandal
    Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States
    J Med Chem 55:9331-45. 2012
    ....
  6. doi Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor
    Jared N Cumming
    Merck Research Laboratories, 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 22:2444-9. 2012
    ..Herein we report SAR development in the S3 and F' subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound...
  7. doi Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists
    Zhong Yue Sun
    Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 19:6801-5. 2009
    ..Various N-heterocyclic substituted aminophenethyl-2-aminobenzothiazole analogs were synthesized to explore the SAR. Isothiourea analogs and ligands with high potency (K(i) 30 nM) have been identified...
  8. doi Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo
    Zhong Yue Sun
    Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States
    J Med Chem 55:489-502. 2012
    ..These designs were applied in the identification of γ-secretase modulators leading to highly efficacious agents for reduction of central nervous system Aβ(42) in various animal models...
  9. doi Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket
    Robert D Mazzola
    Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 18:5809-14. 2008
    ..X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound to the enzyme in the S1'-S3' pocket...
  10. ncbi Structure and activity relationships of tartrate-based TACE inhibitors
    Dansu Li
    Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, 320 Bent Street, Cambridge, MA 02141, United States
    Bioorg Med Chem Lett 20:4812-5. 2010
    ..The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics...
  11. doi Combining NMR and X-ray crystallography in fragment-based drug discovery: discovery of highly potent and selective BACE-1 inhibitors
    Daniel F Wyss
    Merck Research Laboratories, Kenilworth, NJ 07033, USA
    Top Curr Chem 317:83-114. 2012
    ....
  12. doi Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists
    Li Qiang
    Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 20:836-40. 2010
    ..A number of highly potent D(1) antagonists were discovered which have excellent selectivity over other dopamine receptors and improved PK profile compared to SCH 39166...
  13. doi Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators
    Jun Qin
    Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
    Bioorg Med Chem Lett 21:664-9. 2011
    ..Synthesis and SAR of these series are discussed. These compounds represent a new class of γ-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting Aβ(42) production...
  14. doi Iminoheterocycles as gamma-secretase modulators
    John P Caldwell
    Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States
    Bioorg Med Chem Lett 20:5380-4. 2010
    ..Selected compounds exhibit good potency as gamma-secretase modulators, excellent rat pharmacokinetics, and lowering of Abeta42 levels in various in vivo models...