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Volumn 20, Issue 3, 2010, Pages 1059-1062

Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors

Author keywords

Amide; Heterocyclic; Inflammatory; Inhibitor; Kinase; MAP; Oxalyl; p38; Piperidine

Indexed keywords

AMIDE; INDOLE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; PIPERIDINE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA; HETEROCYCLIC COMPOUND; OXALIC ACID DERIVATIVE; PIPERIDINE; PROTEIN KINASE INHIBITOR;

EID: 74049148916     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.031     Document Type: Article
Times cited : (23)

References (26)
  • 16
    • 84925568218 scopus 로고    scopus 로고
    • note
    • Docking studies were conducted using a high-resolution p38α X-ray structure (PDB ID: 1ove). The extra-precision mode of Glide, a ligand-receptor docking tool (Schrodinger, LLC), was used to generate a poses for piperidine indole analog 1. Poses were further filtered by visual inspection.
  • 20
    • 84925561843 scopus 로고    scopus 로고
    • Mavunkel, B. J.; Chakravarty, S.; Perumattam, J. J.; Dugar, S.; Lu, Q.; Liang, X. WO 2000/071535, 2000.
    • Mavunkel, B. J.; Chakravarty, S.; Perumattam, J. J.; Dugar, S.; Lu, Q.; Liang, X. WO 2000/071535, 2000.
  • 21
    • 84925565222 scopus 로고    scopus 로고
    • Mavunkel, B. J, Perumattam, J. J, Lu, Q, Dugar, S, Goyal, B, Wang, D. X, Chakravarty, S, Luedtke, G. R, Nashashibi, I, Tester, R, Tan, X. US Patent Application 2005/288299, 2005
    • Mavunkel, B. J.; Perumattam, J. J.; Lu, Q.; Dugar, S.; Goyal, B.; Wang, D. X.; Chakravarty, S.; Luedtke, G. R.; Nashashibi, I.; Tester, R.; Tan, X. US Patent Application 2005/288299, 2005.
  • 22
    • 84925561842 scopus 로고    scopus 로고
    • Nomura, M.; Takahashi, Y.; Tanase, T.; Miyachi, H.; Tsunoda, M.; Ide, T.; Murakami, K. WO 2000/ 075103, 2000.
    • Nomura, M.; Takahashi, Y.; Tanase, T.; Miyachi, H.; Tsunoda, M.; Ide, T.; Murakami, K. WO 2000/ 075103, 2000.
  • 25
    • 84925561841 scopus 로고    scopus 로고
    • note
    • 50 was determined to be the concentration of compound which reduced the incorporation of ATP into the substrate by 50%, when compared with control reactions containing no inhibitor.
  • 26
    • 84925568217 scopus 로고    scopus 로고
    • The LPS/TNFα Human Whole Blood Assay was run as described in: Mavunkel, B, Dugar, S, Luedtke, G, Tan, X, McEnroe, G. US Patent 6,696,443, 2004
    • The LPS/TNFα Human Whole Blood Assay was run as described in: Mavunkel, B.; Dugar, S.; Luedtke, G.; Tan, X.; McEnroe, G. US Patent 6,696,443, 2004.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.