Zobrazeno 1 - 10
of 51
pro vyhledávání: '"W. Lubisch"'
Autor:
W. Lubisch, Astrid Netz, Wilfried Hornberger, Swati Bhowmik, Liliane Unger, Hervé Geneste, Wolfgang Wernet, Marcel M. van Gaalen, Thorsten Oost, Gisela Backfisch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3828-3831
Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4237a35b3d033a87a33d5c6c4dadf66
https://doi.org/10.1016/j.bmcl.2011.03.012
https://doi.org/10.1016/j.bmcl.2011.03.012
Autor:
Viraj B. Gandhi, Kennan C. Marsh, Vered Klinghofer, Elizabeth H. Fry, Eric F. Johnson, David Frost, Amanda M. Olson, Vincent L. Giranda, Jianchun Gong, Chang H. Park, Yan Luo, Jennifer J. Bouska, Wolfgang Wernet, Roland Grandel, Gui-Dong Zhu, W. Lubisch, Saul H. Rosenberg, Sheela A. Thomas, Yan Shi, Cherrie K. Donawho, Xuesong Liu, Thomas D. Penning, Velitchka Bontcheva-Diaz
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:6965-6975
We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency, as well as cellular potency. These efforts led to the identification of a lead preclinical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17f9dfff4a264cde0e806e9b06f79cf0
https://doi.org/10.1016/j.bmc.2008.05.044
https://doi.org/10.1016/j.bmc.2008.05.044
Autor:
Andreas Haupt, Liliane Unger, Linda L. King, W. Lubisch, Gisela Backfisch, Hervé Geneste, Hans-Jürgen Teschendorf, Jürgen Delzer, Gerd Steiner, Charles W. Hutchins, Wilfried Braje, Wolfgang Wernet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:658-662
The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cb60071b7ee77e5d0fa8b2ac028ca37b
https://doi.org/10.1016/j.bmcl.2005.10.035
https://doi.org/10.1016/j.bmcl.2005.10.035
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2113-2116
Pyrrolylquinoxalinediones carrying aminoalkyl residues were evaluated for affinity to the recombinant, homomeric kainate receptors GluR5, GluR6 and GluR7. Most derivatives preferred binding to GluR5. In particular, the piperazine 6e represents a high
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6602f78ce6edae6d6e84eb81c74cd06c
https://doi.org/10.1016/s0960-894x(02)00335-9
https://doi.org/10.1016/s0960-894x(02)00335-9
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors
Autor:
W. Lubisch, A. Möller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1335-1338
Novel calpain inhibitors derived from phenyl alanine aldehydes or ketoamides carrying a benzoyl residue were prepared and evaluated for their biological potency. A brief structure–activity relationship elucidated the importance of ortho -substitute
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d9b30af711903f94e25355cd3119785
https://doi.org/10.1016/s0960-894x(02)00176-2
https://doi.org/10.1016/s0960-894x(02)00176-2
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2187-2191
Calpain inhibitors which are derived from piperidine carboxamides in the P2 region were prepared and evaluated for mu-calpain inhibition. In particular, the keto amides 11f and 11j have Ki of 30 and 9 nM and display a more than 100-fold selectivity o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bce45ac13e45c730fa5c5f9963a3c35a
https://doi.org/10.1016/s0960-894x(00)00430-3
https://doi.org/10.1016/s0960-894x(00)00430-3
Autor:
W. Lubisch, H. G. Lemaire, H. J. Teschendorf, Berthold Behl, T. Höger, D. Seemann, H. Lehmann, G. Groß, Wolfgang Löscher, H. P. Hofmann
Publikováno v:
European Journal of Neuroscience. 11:250-262
Antagonists at the ionotropic non-NMDA [AMPA (amino-methyl proprionic acid)/kainate] type of glutamate receptors have been suggested to possess several advantages compared to NMDA (N-methyl-D-aspartate) receptor antagonists, particularly in terms of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::34dc3705af31441aaeac7c99937eee85
https://doi.org/10.1046/j.1460-9568.1999.00432.x
https://doi.org/10.1046/j.1460-9568.1999.00432.x
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2441-2446
Pyrrolylquinoxalinediones carrying carboxylates at the pyrrole side-chain were synthesized and evaluated for AMPA receptor binding and for selectivity over other glutamate receptors. Particularly dicarboxy derivatives represent selective and highly p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::46e331beb0f9acd6e3d1e78af7c1d6c5
https://doi.org/10.1016/s0960-894x(97)00428-9
https://doi.org/10.1016/s0960-894x(97)00428-9
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1101-1106
Pyrrolylquinoxalinediones were synthesized to elucidate the value of pyrrolic substitution pattern on AMPA receptor binding. We discovered that amide and urea residues at the 3′-position at pyrrol ring favor affinity to AMPA receptor. Particularly,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::70ed348daadb44218193ead7eb717f56
https://doi.org/10.1016/s0960-894x(97)00170-4
https://doi.org/10.1016/s0960-894x(97)00170-4
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2887-2892
Pyrrolylquinoxalinediones were synthesized and their affinities for the AMPA receptor were determined. Most compounds showed moderate to good affinities. The acetic acid derivative 8b exhibited a Ki value of 70 nM and was equipotent to NBQX 1. Struct
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b9cc5affc9da768662a61f05a8a9638a
https://doi.org/10.1016/s0960-894x(96)00534-3
https://doi.org/10.1016/s0960-894x(96)00534-3