Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Bernhard Neises"'
Autor:
Hans Matter, Wilfried Schwab, Günter Dr. Billen, Theo Wollmann, Werner Thorwart, Denis Barbier, Bernhard Neises, Haase Burkhard, Klaus-Ulrich Weithmann, Manfred Schudok
Publikováno v:
Bioorganic & Medicinal Chemistry. 10:3529-3544
The design, synthesis and structure–activity relationship (SAR) of a series of nonpeptidic 2-arylsulfonyl-1,2,3,4-tetrahydro-isoquinoline-3-carboxylates and-hydroxamates as inhibitors of the matrix metalloproteinase human neutrophil collagenase (MM
Autor:
Hans Matter, Herman Schreuder, Haase Burkhard, Manfred Schudok, Günter Dr. Billen, Denis Barbier, Werner Thorwart, Klaus Ulrich Dr Weithmann, Bernhard Neises, Volker Brachvogel, Petra Lönze, Wilfried Schwab
Publikováno v:
Journal of Medicinal Chemistry. 42:1908-1920
A set of 90 novel 2-(arylsulfonyl)-1,2,3, 4-tetrahydroisoquinoline-3-carboxylates and -hydroxamates as inhibitors of the matrix metalloproteinase human neutrophil collagenase (MMP-8) was designed, synthesized, and investigated by 3D-QSAR techniques (
Publikováno v:
Nucleosides and Nucleotides. 15:1469-1479
The phosphorylation of thymidine-5′-monophosphate (dTMP) by chick embryo liver thymidylate kinase (Km (dTMP) =1.2 μM) was inhibited by the 5′-monophosphate derivatives of 5-bromo-2′-deoxyuridine (5-Br-dUMP), 5-iodo-2′-deoxyuridine (5-I-dUMP)
Autor:
J.M. Altenburger, V. Van Dorsselaer, Daniel Schirlin, S. Baltzer, C. Weill, Gary A. Flynn, J.M. Remy, Bernhard Neises, F. Weber, Celine Tarnus
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:253-258
Structure-activity relationship and concept evaluation studies have yielded short and unexpectedly potent inhibitors of HIV-1 protease of the difluorostatione type.
Autor:
C. Weill, Bernhard Neises, Celine Tarnus, Daniel Schirlin, F. Weber, S. Baltzer, J.M. Remy, Gary A. Flynn, J.M. Altenburger, V. Van Dorsselaer
Publikováno v:
ChemInform. 24
Publikováno v:
ChemInform. 28
Publikováno v:
Liebigs Annalen der Chemie. 1990:1-6
The synthesis of α-amino mono-, di-, and trifluoromethyl and difluoromethylene ketones and their derivatives is described. A one-pot sequence related to the Dakin-West reaction starts from amino acids and gives the corresponding fluorinated ketone a
Autor:
Bernhard Neises, Michael R. Angelastro, Shujaath Mehdi, Philippe Bey, Eugene L Giroux, Joseph P. Burkhart, Michael Kolb, Daniel Schirlin, Norton P. Peet
Publikováno v:
Journal of Medicinal Chemistry. 33:394-407
Comparison of MeO-Suc-Val-Pro-Phe-CO2Me (29) and MeO-Suc-Ala-Ala-Pro-Phe- CO2Me (25) with their corresponding trifluoromethyl ketones 9a and 9b, respectively, in rat and human neutrophil cathepsin G assays showed the alpha-keto esters to be more pote
Autor:
Herman Schreuder, Bernhard Neises, L.W. Kutcher, Joseph P. Burkhart, Shujaath Mehdi, Chantal Tardif, J. A. Malikayil, Norton P. Peet, Gerald L. Schatzman, Robert J. Broersma
Publikováno v:
Biochemistry. 36(5)
An inhibitor of alpha-thrombin was designed on the basis of the X-ray crystal structures of thrombin and trypsin. The design strategy employed the geometric and electrostatic differences between the specificity pockets of the two enzymes. These diffe
Autor:
Robert J. Broersma, Eileen F. Heminger, J.M. Remy, C. Lintz, L.W. Kutcher, F. Piriou, Celine Tarnus, Bernhard Neises
Publikováno v:
Bioorganicmedicinal chemistry. 3(8)
Fluorinated ketone thrombin inhibitors based on the peptide sequence methyl-( d )-Phe-Pro-Arg-CF 2 R were synthesized: MDL 73,446 (1, R = F); MDL 73,775 (2, R = CF 3 ); and MDL 75,579 (3, R = CH 2 CH 2 CH 3 ). These were shown to be highly effective,