Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Obbe P. Zuiderveld"'
Autor:
Heribert Arnhof, Dirk Scharn, Julia Dobler, Katharina Stachurski, Obbe P. Zuiderveld, Henry F. Vischer, Eric E. J. Haaksma, Moriz Mayer, Saskia Nijmeijer, Sabine Schultes, Rob Leurs, Chris de Graaf, Iwan J. P. de Esch, Harald Engelhardt
Publikováno v:
Journal of Medicinal Chemistry, 2013(56), 4264-4276. American Chemical Society
Engelhardt, H, Schultes, S, de Graaf, C, Nijmeijer, S, Vischer, H F, Zuiderveld, O B, Dobler, J, Stachurski, K, Mayer, M, Arnhof, H, Scharn, D, Haaksma, E J J, de Esch, I J P & Leurs, R 2013, ' Bispyrimidines as potent histamine H4 receptor ligands: delineation of structure activity relationships and detailed H4 receptor binding mode ', Journal of Medicinal Chemistry, vol. 2013, no. 56, pp. 4264-4276 . https://doi.org/10.1021/jm301886t
Engelhardt, H, Schultes, S, de Graaf, C, Nijmeijer, S, Vischer, H F, Zuiderveld, O B, Dobler, J, Stachurski, K, Mayer, M, Arnhof, H, Scharn, D, Haaksma, E J J, de Esch, I J P & Leurs, R 2013, ' Bispyrimidines as potent histamine H4 receptor ligands: delineation of structure activity relationships and detailed H4 receptor binding mode ', Journal of Medicinal Chemistry, vol. 2013, no. 56, pp. 4264-4276 . https://doi.org/10.1021/jm301886t
The basic methylpiperazine moiety is considered a necessary substructure for high histamine H4 receptor (H4R) affinity. This moiety is however also the metabolic hot spot for various classes of H4R ligands (e.g., indolcarboxamides and pyrimidines). W
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10f837a95333a3e534589588754b1af9
https://doi.org/10.1021/jm301886t
https://doi.org/10.1021/jm301886t
Autor:
Iwan J. P. de Esch, Obbe P. Zuiderveld, Rob Leurs, Harald Engelhardt, Eric E. J. Haaksma, Luc Roumen, Sabine Schultes, Chris de Graaf
Publikováno v:
ChemMedChem, 8(1), 49-53. John Wiley and Sons Ltd
Schultes, S, Engelhardt, H, Roumen, L, Zuiderveld, O P, Haaksma, E J J, de Esch, I J P, Leurs, R & de Graaf, C 2013, ' Combining quantum mechanical ligand conformation analys is and protein modeling to elucidate GPCR–ligand binding modes ', ChemMedChem, vol. 8, no. 1, pp. 49-53 . https://doi.org/10.1002/cmdc.201200412
Schultes, S, Engelhardt, H, Roumen, L, Zuiderveld, O P, Haaksma, E J J, de Esch, I J P, Leurs, R & de Graaf, C 2013, ' Combining quantum mechanical ligand conformation analys is and protein modeling to elucidate GPCR–ligand binding modes ', ChemMedChem, vol. 8, no. 1, pp. 49-53 . https://doi.org/10.1002/cmdc.201200412
SAR beyond protein-ligand interactions: By combining structure-affinity relationships, protein-ligand modeling studies, and quantum mechanical calculations, we show that ligand conformational energies and basicity play critical roles in ligand bindin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17a3e734a647f0eb257517e2f7c4a13f
https://doi.org/10.1002/cmdc.201200412
https://doi.org/10.1002/cmdc.201200412
Autor:
Herman D. Lim, Iwan J. P. de Esch, Rogier A. Smits, Karin Bessembinder, Sebastiaan Kuhne, Maikel Wijtmans, Tiffany van der Meer, Rob Leurs, Obbe P. Zuiderveld
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:461-467
The histamine H(4) receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H(4)R ligands, a low affinity isoquinoline fragment was optimized to 7-(fu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f09c40333caa3790926e9d01ebb91ad
https://doi.org/10.1016/j.bmcl.2011.10.104
https://doi.org/10.1016/j.bmcl.2011.10.104
Autor:
Linda Silvestri, Rogier A. Smits, Sarah C. R. Lummis, Andrew J. Thompson, Rob Leurs, Jacqueline E. van Muijlwijk-Koezen, Saskia Hulscher, Chris de Graaf, Obbe P. Zuiderveld, Gerdien E. de Kloe, Henry F. Vischer, Mark H.P. Verheij, Saskia Nijmeijer, Iwan J. P. de Esch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters
Graphical abstract
A fragment library was screened against the G protein-coupled histamine H4 receptor (H4R) and the ligand-gated ion channel serotonin 5-HT3A (5-HT3AR). Interestingly, significant overlap was found between H4R and 5-HT3AR hit se
A fragment library was screened against the G protein-coupled histamine H4 receptor (H4R) and the ligand-gated ion channel serotonin 5-HT3A (5-HT3AR). Interestingly, significant overlap was found between H4R and 5-HT3AR hit se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d52e42d222c6c62125893e7bac70bb4a
https://doi.org/10.1016/j.bmcl.2011.06.123
https://doi.org/10.1016/j.bmcl.2011.06.123
Publikováno v:
Archiv der Pharmazie. 341:762-773
A series of 1-benzyl-4-(3-aminopropyloxy)piperidine and 1-benzyl-4-(5-aminopentyloxy)piperidine derivatives has been prepared. The 1-benzyl-4-hydroxypiperidine derivatives obtained were evaluated for their affinities at recombinant human histamine H(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8ca7b0a22a83f67488625e1429b3ccb
https://doi.org/10.1002/ardp.200800070
https://doi.org/10.1002/ardp.200800070
Autor:
T.L. ter Laak, Obbe P. Zuiderveld, Thijs Beuming, Rob Leurs, Uli Hacksell, Remko A. Bakker, M. Edelbroek, Henk Timmerman, D. M. Weiner, Mark R. Brann
Publikováno v:
Bakker, R A, Weiner, D M, ter Laak, T L, Beuming, T, Zuiderveld, O P, Edelbroek, M, Hacksell, U, Timmerman, H, Brann, M R & Leurs, R 2004, ' 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist ', Molecular Pharmacology, vol. 65, no. 3, pp. 538-49 . https://doi.org/10.1124/mol.65.3.538
Molecular Pharmacology, 65(3), 538-49. American Society for Pharmacology and Experimental Therapeutics
Molecular Pharmacology, 65(3), 538-49. American Society for Pharmacology and Experimental Therapeutics
The human histamine H1 receptor (H1R) is an important, well characterized target for the development of antagonists to treat allergic conditions. Many neuropsychiatric drugs are known to potently antagonize the H1R, thereby producing some of their si
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74bb3dfd8c92512e5e15cadeb7a45e87
https://doi.org/10.1124/mol.65.3.538
https://doi.org/10.1124/mol.65.3.538
Autor:
Obbe P. Zuiderveld, Roeland C. Vollinga, Ruengwit Kitbunnadaj, Henk Timmerman, Rob Leurs, Anthony L. Spek, Marie-France Deltent, Martin Lutz, Iwan J. P. de Esch, Emile Cavoy, Remko A. Bakker, Wiro M. P. B. Menge
Publikováno v:
Kitbunnadaj, R, Zuiderveld, O P, De Esch, I J, Vollinga, R C, Bakker, R A, Lutz, M, Spek, A L, Cavoy, E, Deltent, M F, Menge, W M P B, Timmerman, H & Leurs, R 2003, ' Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists ', Journal of Medicinal Chemistry, vol. 46, no. 25, pp. 5445-57 . https://doi.org/10.1021/jm030905y
Journal of Medicinal Chemistry, 46(25), 5445-57. American Chemical Society
Journal of Medicinal Chemistry, 46(25), 5445-57. American Chemical Society
Immepip, a conformationally constrained analogue of the histamine congener imbutamine, shows high affinity and functional activity on the human H(3) receptor. Using histamine and its homologues as prototypes, other rigid analogues containing either a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03c69a86f54b62fea7f4ba6476f02e84
https://doi.org/10.1021/jm030905y
https://doi.org/10.1021/jm030905y
Autor:
Seiichiroh Takashima, Martine J. Smit, Tomonari Imazu, Remko A. Bakker, Yumiko Yamamoto, Rob Leurs, Takushi Kurihara, Yasuhiko Sakamoto, Takeshi Hashimoto, Atsushi Yamatodani, Lisa Araki, Obbe P. Zuiderveld, Shinya Harusawa
Publikováno v:
Hashimoto, T, Harusawa, S, Araki, L, Zuiderveld, O P, Smit, M J, Imazu, T, Takashima, S, Yamamoto, Y, Sakamoto, Y, Kurihara, T, Leurs, R, Bakker, R A & Yamatodani, A 2003, ' A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5-[1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine ', Journal of Medicinal Chemistry, vol. 46, no. 14, pp. 3162-5 . https://doi.org/10.1021/jm0300025
Journal of Medicinal Chemistry, 46(14), 3162-5. American Chemical Society
Journal of Medicinal Chemistry, 46(14), 3162-5. American Chemical Society
A series of 16 compounds related to chiral 4(5)-(5-aminomethyltetrahydrofuran-2-yl)imidazoles (1) have been designed, synthesized, and examined in vitro by radioligand displacement studies and functional assays for both the human H(3)- and H(4)-recep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a086139f383e29104c6615adb48a6018
https://doi.org/10.1021/jm0300025
https://doi.org/10.1021/jm0300025
Publikováno v:
Il Farmaco. 54:684-694
New 2-(1-Piperazinyl)- and 2-(hexahydro-1 H -1,4-diazepin-1-yl)benzothiazoles were prepared and tested as H 1 - and H 3 -receptor antagonists. A number of compounds showed weak H 1 -antagonistic activity, with p A 2 values ranging from 5.5 to 6.1. Th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::657c31adfe2112812b0eb4dafdb6b95c
https://doi.org/10.1016/s0014-827x(99)00081-6
https://doi.org/10.1016/s0014-827x(99)00081-6
Publikováno v:
Il Farmaco. 54:533-541
New 2-[2-(phenylamino)thiazol-4-yl]ethanamine and 2-(2-benzhydrylthiazol-4-yl)ethanamine derivatives were prepared and tested in vitro as H1 receptor antagonists. The compounds with 2-phenylamino substitution with meta-halide substituents at the phen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e955d1212d3cd122abfbe937a313fbc5
https://doi.org/10.1016/s0014-827x(99)00060-9
https://doi.org/10.1016/s0014-827x(99)00060-9