Research Topics
| Luping LiuSummaryAffiliation: Merck Research Laboratories Country: USA Publications
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Detail Information
Publications
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitorsLuping Liu
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 13:3979-82. 2003..Modification of N-1 aryl and C-6 arylsulfide in 3,4-dihydropyrido(3,2-d)pyrimidone analogues for the interaction with the hydrophobic pockets in p38 active site is also discussed...
p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffoldSwaminathan R Natarajan
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 16:5468-71. 2006..Compound 16 reduced inflammation in animal disease models at EC(50) doses as low as 0.2mpk...
The three-dimensional structure of MAP kinase p38beta: different features of the ATP-binding site in p38beta compared with p38alphaSangita B Patel
Department of Global Structural Biology, Merck Research Laboratory, Rahway, NJ 07065, USA
Acta Crystallogr D Biol Crystallogr 65:777-85. 2009..This difference in size between the two pockets could be exploited in order to achieve selectivity...
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinonesJianming Bao
Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 16:64-8. 2006..They also displayed excellent PK profiles across three animal species. Quinolinone at 10 mpk showed comparable oral efficacy to that of dexamethasone at 1 mpk in a murine collagen-induced arthritis model...
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinaseJohn E Stelmach
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 13:277-80. 2003..58 microM h)...
