Zobrazeno 1 - 10
of 32
pro vyhledávání: '"David G. Sawutz"'
Autor:
Kevin N. Winzenberg, Teresa Cablewski, Abdelselam Ali, Roger M. Sargent, David G. Sawutz, Ashit K. Ganguly, Craig L. Francis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4160-4163
A series of 2-phenylimidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for their in vitro anthelmintic activity against Haemonchus contortus. The most active compounds had in vitro LD99 values of 30 nM, which is comparable to that of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::060cbaef95d2a075fc9f23dbd8c37f1d
https://doi.org/10.1016/j.bmcl.2011.05.096
https://doi.org/10.1016/j.bmcl.2011.05.096
Autor:
Petr Fisara, Roger M. Sargent, Adam G. Meyer, David G. Sawutz, Andris J. Liepa, Marianne Bliese, Timothy Michael Altamore, Oahn Nguyen, David A. Winkler, Angela Ziebell, Abdelselam Ali, Kevin N. Winzenberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:252-255
A series of novel 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilide derivatives have shown significant in vitro parasiticidal activity against the ectoparasites Ctenocephalides felis and Rhipicephalus sanguineus. A number of these compo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::103d7e3dcd3ba7b7333258404f1206fb
https://doi.org/10.1016/j.bmcl.2007.10.090
https://doi.org/10.1016/j.bmcl.2007.10.090
Autor:
David G. Sawutz, David A. Winkler, Abdelselam Ali, Roger M. Sargent, John S. Wilkie, Ruth C. J. Woodgate, Marianne Bliese, Simon Saubern, Kevin N. Winzenberg, Jo Anne M Rasmussen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:993-997
A series of 2-phenyl-3-(1H-pyrrol-2-yl)acrylonitrile derivatives were synthesized and evaluated for in vitro activity against the endoparasite Haemonchus contortus and the ectoparasite Ctenocephalides felis. Some compounds had significant in vitro ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08bf81bffbb5833ee5728f05c3842004
https://doi.org/10.1016/j.bmcl.2006.11.043
https://doi.org/10.1016/j.bmcl.2006.11.043
Publikováno v:
Immunopharmacology. 35:27-39
The binding characteristics of the sigma ligand [3H]1.3-di(2-tolyl)guanidine (DTG) were investigated in membranes prepared from the Jurkat T cell line. Binding was saturable with a KD of 56 +/- 3 nM and a Bmax of 11706 +/- 3173 fmol/mg protein (n = 3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::095d6562a990e168e234dff52b3def71
https://doi.org/10.1016/0162-3109(96)00107-5
https://doi.org/10.1016/0162-3109(96)00107-5
Autor:
J D Schroeder, E McAvoy, Y Baine, C R Shah, Adi Treasurywala, Joseph Guiles, M F Stansberry, David G. Sawutz, William F. Michne, Carolyn A. Weigelt
Publikováno v:
Journal of Medicinal Chemistry. 38:2557-2569
The preparation of a series of quinazoline-2,4-diones, 1-3, and pyrrolo[3,4-d]pyrimidine-2,4-diones, 4-8 is described. A small number of quinazolinedione analogs were identified from random screening to possess low micromolar (1.3-4.4 microM) potency
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe6d3cb0617aa1059e800ee11097fcbb
https://doi.org/10.1021/jm00014a009
https://doi.org/10.1021/jm00014a009
Publikováno v:
Canadian Journal of Physiology and Pharmacology. 73:805-811
A series of competitive, nonpeptide bradykinin receptor antagonists based on an α-amino acid scaffold have been developed and biologically characterized. The lead compound in the series, WIN 64338, demonstrates competitive inhibition of bradykinin-m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce413a213753e54317d87ab812be3c06
https://doi.org/10.1139/y95-109
https://doi.org/10.1139/y95-109
Autor:
Su Wang, Deborah Ann Miller, Wen Xie, Marian Kelley, David G. Sawutz, John Reid, Muhmut Miski, Roland E. Dolle, Jay Sarup, Bruce Gauvin, Connie R. Faltynek
Publikováno v:
Drug Development Research. 34:344-352
The protein tyrosine kinase p56Ick, which is expressed predominantly in lymphocytes, plays a critical role in optimal T cell activation through the T cell antigen receptor. An approach is presented for the discovery of selective p56Ick inhibitors, wh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::060e258900dbe15ca2a3ba0057cb49c7
https://doi.org/10.1002/ddr.430340406
https://doi.org/10.1002/ddr.430340406
Autor:
Awad Mohamed M A, Wayne T. Houck, Hoyer Denton W, Peter R. Seoane, Roland E. Dolle, David G. Sawutz, Salvino Joseph M
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:367-370
Angiotensin converting enzyme (ACE) degrades both angiotensin II and bradykinin. Accordingly, we hypothesize that ACE inhibitors can serve as models to design antagonists for the bradykinin receptor. The potent ACE inhibitor Quinapril was modified to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e8e4baae45845d6121a553360438103d
https://doi.org/10.1016/0960-894x(95)00037-t
https://doi.org/10.1016/0960-894x(95)00037-t
Autor:
Patricia Mauvais, Jay Sarup, Deborah Ann Miller, Susan Hoekstra, Bruce Gauvin, Paul Juniewicz, Su Wang, Ruth Lehr, Wen Xie, John Reid, Dennis J. Murphy, David G. Sawutz, Connie R. Faltynek
Publikováno v:
Journal of Enzyme Inhibition. 9:111-122
A new p56idk tyrosine kinase inhibitor WIN 61651 [1,4-dihydro-7-(4-methyl-1-piperizinyl)-1-(4-(4-methyl-1-piperizinyl))phenyl-4-oxo-3-quinolinecarboxamide) is described. WIN 61651, which is competitive with AP, demonstrates selectivity for the lympho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bb2a63c2919629141757ffda1fb3e78
https://doi.org/10.3109/14756369509042811
https://doi.org/10.3109/14756369509042811
Publikováno v:
Journal of Receptors and Signal Transduction. 15:829-846
AMPA receptors may play an important role in acute and chronic neurodegenerative diseases. An assay for the specific binding of [3H]-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) to receptors in membranes from post-mortem human brain is d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02331173c1b6234fa90971d8c74be7a9
https://doi.org/10.3109/10799899509049860
https://doi.org/10.3109/10799899509049860