Adam M Gilbert

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
    Adam M Gilbert
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 17:1189-92. 2007
  2. ncbi Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors
    Adam M Gilbert
    Department of Chemical and Screening Sciences, Wyeth Research, 401N Middletown Road, Pearl River, NY 10945, USA
    Bioorg Med Chem Lett 14:37-41. 2004
  3. ncbi Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane
    Adam M Gilbert
    Chemical and Screening Sciences, Wyeth Research, 401N Middletown Road, Pearl River, NY 10945, USA
    Bioorg Med Chem Lett 14:515-8. 2004
  4. ncbi Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity
    Adam M Gilbert
    Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965 1215, USA
    Bioorg Med Chem Lett 14:5281-4. 2004
  5. doi Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies
    Adam M Gilbert
    Medicinal Chemistry, Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 20:636-9. 2010
  6. doi Hit to lead studies on (hetero)arylpyrimidines--agonists of the canonical Wnt-beta-catenin cellular messaging system
    Adam M Gilbert
    Chemical Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, United States
    Bioorg Med Chem Lett 20:366-70. 2010
  7. ncbi Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase
    Adam M Gilbert
    Chemical and Screening Sciences and Infectious Diseases Research, Wyeth, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 49:6027-36. 2006
  8. doi N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2)
    Adam M Gilbert
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 18:6454-7. 2008
  9. doi Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies
    Matthew G Bursavich
    Medicinal Chemistry, Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 20:2586-90. 2010
  10. ncbi Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
    Matthew G Bursavich
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 17:1185-8. 2007

Detail Information

Publications16

  1. ncbi 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
    Adam M Gilbert
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 17:1189-92. 2007
    ..Compound 12 is noteworthy in that it has an ADAMTS-5 IC50: 1.1 microM and shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1)...
  2. ncbi Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors
    Adam M Gilbert
    Department of Chemical and Screening Sciences, Wyeth Research, 401N Middletown Road, Pearl River, NY 10945, USA
    Bioorg Med Chem Lett 14:37-41. 2004
    ..1 microM, 16: 1.5 microM, 18: 0.27 microM) and moderate antibacterial activity (MICs: 12.5-50 microM) against B. subtilis, E. faecalis ATCC, E. faecalis VRE and S. pneumo+...
  3. ncbi Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane
    Adam M Gilbert
    Chemical and Screening Sciences, Wyeth Research, 401N Middletown Road, Pearl River, NY 10945, USA
    Bioorg Med Chem Lett 14:515-8. 2004
    ..A 3-benzothiophene analogue of 4 (30) was synthesized which possesses potent 5-HT(1A) affinity and especially good selectivity over both alpha(1) and 5-HT-T...
  4. ncbi Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity
    Adam M Gilbert
    Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965 1215, USA
    Bioorg Med Chem Lett 14:5281-4. 2004
    ..2nM, 25: 0.54nM, 27: 0.38nM) and good 5-HT(1A) affinity/antagonism (5-HT(1A)K(i), [(35)S]GTPgammaS: E(max) (%): 21: 111.1nM, 0%; 25: 173.2nM, 0%; 27: 107nM, 0%)...
  5. doi Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies
    Adam M Gilbert
    Medicinal Chemistry, Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 20:636-9. 2010
    ..Signaling through the PI3K pathway was confirmed via inhibition of phospho-AKT in MDA-361 cells...
  6. doi Hit to lead studies on (hetero)arylpyrimidines--agonists of the canonical Wnt-beta-catenin cellular messaging system
    Adam M Gilbert
    Chemical Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, United States
    Bioorg Med Chem Lett 20:366-70. 2010
    ..Two examples 1 and 25 show in vivo osteogenic activity in a mouse calvaria model. One example 1 is shown to activate non-phosphorylated beta-catenin formation in bone...
  7. ncbi Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol-3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase
    Adam M Gilbert
    Chemical and Screening Sciences and Infectious Diseases Research, Wyeth, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 49:6027-36. 2006
    ..Docking studies using FLO and PharmDock produced several binding orientations for these molecules in the MurB active site...
  8. doi N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2)
    Adam M Gilbert
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 18:6454-7. 2008
    ..This series of compounds represents progress towards selective ADAMTS-5 inhibitors as disease modifying osteoarthritis agents...
  9. doi Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies
    Matthew G Bursavich
    Medicinal Chemistry, Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 20:2586-90. 2010
    ..Compounds show activity in multiple cellular proliferation assays with signaling through the PI3K pathway confirmed via phospho-Akt inhibition in PC-3 cells...
  10. ncbi Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
    Matthew G Bursavich
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 17:1185-8. 2007
    ..This series of compounds represents steps toward a metalloprotease inhibitor as a disease-modifying osteoarthritis drug...
  11. ncbi Use of structure-based drug design approaches to obtain novel anthranilic acid acyl carrier protein synthase inhibitors
    Diane Joseph-McCarthy
    Wyeth Research, 200 CambridgePark Drive, Cambridge, Massachusetts 01240, USA
    J Med Chem 48:7960-9. 2005
    ..Four X-ray complex structures of representative anthranilic acid ligands bound to AcpS are described in detail...
  12. ncbi 5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2)
    Matthew G Bursavich
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 17:5630-3. 2007
    ..This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug...
  13. doi Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors
    Aranapakam M Venkatesan
    Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States
    Bioorg Med Chem Lett 20:653-6. 2010
    ..These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of Akt at T308...
  14. doi (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate
    Jeffrey C Pelletier
    Chemical Sciences, Drug Safety and Metabolism, Wyeth Research, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 52:6962-5. 2009
    ..Compound 5 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration...
  15. ncbi Expedient parallel synthesis of 2-amino-4-heteroarylpyrimidines
    Matthew G Bursavich
    Exploratory Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    Org Lett 7:4113-6. 2005
    ..A series of potentially biologically active analogues have been synthesized in two parallel steps to afford focused arrays...
  16. ncbi Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers
    Adam M Gilbert
    Chemical Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965 1299, and Bone Metabolism and Osteoporosis Research, Wyeth Research, 145 King of Prussia Road, Radnor, Pennsylvania 19087 4588
    J Med Chem 45:2342-5. 2002
    ..These two series are notable examples of small molecules that act as CT-inducers, a method to potentially treat bone loss diseases...