Zobrazeno 1 - 10
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pro vyhledávání: '"Maynard, George D."'
Autor:
Kehne, John H., Maynard, George D.
Publikováno v:
In Drug Discovery Today: Therapeutic Strategies 2008 5(3):161-168
Akademický článek
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Akademický článek
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Autor:
S. A. Shatzer, Robert W. Knippenberg, Deborah E. Logan, Hector Esteve, Maynard George D, Lily Hsieh, Karl Olsen, Kudlacz Elizabeth M
Publikováno v:
International Archives of Allergy and Immunology. 115:169-178
Background: Histamine is a critical mediator of immediate hypersensitivity reactions. Sensory neuropeptides, such as substance P (SP), may also contribute to acute inflammatory responses. A compound which antagonizes both H1 and NK-1 receptors, such
Autor:
Maynard George D, Kenneth T. Stewart, Deborah E. Logan, Larry D. Bratton, Kane John M, Kudlacz Elizabeth M, Robert W. Knippenberg, Braulio Santiago, Amy M. Farrell, Burkholder Timothy P, S. A. Shatzer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2819-2824
A series of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity has been prepared. Factors affecting receptor binding affinities and oral activity in this series are described.
Autor:
S. A. Shatzer, Maynard George D, Larry D. Bratton, Kudlacz Elizabeth M, Roy J. Vaz, John M. Kane, Robert W. Knippenberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2825-2830
Support for the conformation used in the design of a series of 4-(1 H -benzimidazole-2-carbonyl)piperidines with dual histamine H 1 /tachykinin NK 1 receptor antagonist activity has been presented. Comparative Molecular Field Analysis(CoMFA) for both
Autor:
Julie L. Geary, Melinda A. Correll, J. Chuck Poole, Xiao-Gao Liu, Larry D. Bratton, Fred E. Boyer, Thomas N. Thompson, Teng-Man Chen, Arun K. Mandagere, Bryan K. Jones, Kin-Kai Hwang, Mark E. Webster, Robert W. Knippenberg, Maynard George D, Stephen W. Horgan, Deborah E. Logan, Tieu-Binh Le, Kudlacz Elizabeth M, David L. Wenstrup, Burkholder Timothy P, Raymond S. Gross, David W. Freund
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2531-2536
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors.1 Here we report the synthesis and structure-activity relationships for a series of analogs of M
Autor:
Tieu-Binh Le, S. A. Shatzer, Burkholder Timothy P, Maynard George D, Stephen W. Horgan, Kudlacz Elizabeth M, Robert W. Knippenberg, Mark E. Webster
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:951-956
We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 (IC50=3.11 nM) and NK2 (IC50=8.40 nM) receptors. The chemical synthesis of MDL 105,212 and the SAR of a series of racemi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:753-756
The synthesis of 4-( N -methoxy- N -methylcarboxamido)-1-piperidinecarboxylic acid 1,1-dimethylethyl ester ( 5 ) is described. Reaction of this intermediate with 2-lithiobenzothiazole followed by deprotection and N-alkylation yields a series of 4-(2-