Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Danielle L, Aubele"'
Autor:
Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v:
Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c5b61686f688dd0abd9c5edac66d7201
https://doi.org/10.1021/jm301741t
https://doi.org/10.1021/jm301741t
Autor:
Kevin P. Quinn, Marc Adler, Gary Probst, Albert W. Garofalo, Anh P. Truong, Danny Tam, Erich Goldbach, Danielle L. Aubele, Maurizio Franzini, David Chian, Grace Kwong, Xiaocong M. Ye, Zhao Ren, Hing L. Sham, Lany Ruslim, Pearl Tanaka, Elizabeth F. Brigham, Ruth Motter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1974-1977
Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is increased by pathogenic mutations. Inhibition of LRRK2 kinase activity has therefore emerged as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb913a2423fe06417cb2ecd3e68cdbb8
https://doi.org/10.1016/j.bmcl.2013.02.041
https://doi.org/10.1016/j.bmcl.2013.02.041
Autor:
Anh P. Truong, Shawn Gauby, Pam Santiago, Xiaocong M. Ye, Danielle L. Aubele, Marc Adler, Danny Tam, Albert W. Garofalo, Maurizio Franzini, Hing L. Sham, Erich Goldbach, Gary Probst, Zhao Ren, Kevin P. Quinn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1967-1973
Leucine-rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c53cd9ad2f6df27825036916b0099a94
https://doi.org/10.1016/j.bmcl.2013.02.043
https://doi.org/10.1016/j.bmcl.2013.02.043
Autor:
Colin Lorentzen, Maurizio Franzini, Anh P. Truong, R. Jeffrey Neitz, Marc Adler, Danielle L. Aubele, Pam Santiago, Hing L. Sham, Albert W. Garofalo, Simeon Bowers, Xiaocong M. Ye, Danny Tam, Kevin P. Quinn, Gary Probst, Zhao Ren, Erich Goldbach
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:71-74
Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fde1033b8be37d0cb96bbb6c3ba3646b
https://doi.org/10.1016/j.bmcl.2012.11.021
https://doi.org/10.1016/j.bmcl.2012.11.021
Autor:
Chris M. Semko, Danielle L. Aubele, Guriqbal S. Basi, Wes Zmolek, Gary Probst, Matthew N. Mattson, Elizabeth F. Brigham, Erich Goldbach, Karina Wong, William A Wallace, John-Michael Sauer, Hing L. Sham, Lan K. Nguyen, Michael P. Bova, Andrei W. Konradi, Albert W. Garofalo, Susanna S. Hemphill, Darren B. Dressen, Kevin P. Quinn, Minghua Sun, Anh P. Truong, Simeon Bowers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5791-5794
The structure–activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate β-amyloid peptide synthesis via γ-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c797a2f9e3d425d83f37dc2fbd3a6ac
https://doi.org/10.1016/j.bmcl.2011.08.008
https://doi.org/10.1016/j.bmcl.2011.08.008
Autor:
John-Michael Sauer, Michael P. Bova, Michael A. Pleiss, Danielle L. Aubele, Elizabeth F. Brigham, Kevin P. Quinn, Balazs G. Szoke, Jennifer Marugg, Wes Zmolek, Andrei W. Konradi, Erich Goldbach, William A Wallace, Guriqbal S. Basi, Martin L. Neitzel, Jacek Jagodzinski, Susanna S. Hemphill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3715-3720
Herein we describe the structure-activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1, highlighting affects on the potency of γ-secretase inhibition, selectivity for the inhibition of APP vers
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27cb6eff90f380877a438f6c83cf02d4
https://doi.org/10.1016/j.bmcl.2011.04.079
https://doi.org/10.1016/j.bmcl.2011.04.079
Autor:
Xiaocong M, Ye, Andrei W, Konradi, Jenifer, Smith, Danielle L, Aubele, Albert W, Garofalo, Jennifer, Marugg, Marty L, Neitzel, Chris M, Semko, Hing L, Sham, Minghua, Sun, Anh P, Truong, Jing, Wu, Hongbin, Zhang, Erich, Goldbach, John-Michael, Sauer, Elizabeth F, Brigham, Michael, Bova, Guriqbal S, Basi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3502-3506
Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::864d25ea6d9242d49f72de8a339b07d1
https://doi.org/10.1016/j.bmcl.2010.04.148
https://doi.org/10.1016/j.bmcl.2010.04.148
Publikováno v:
Tetrahedron: Asymmetry. 16:3570-3578
Oxidatively generated oxocarbenium ions are shown to be effective promoters of polyepoxide cascade cyclization reactions to form polyether compounds. The reaction conditions are neutral, ensuring that background acid-mediated processes are not operat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2e16b1817a887f3fd7e6ed89ea990fd8
https://doi.org/10.1016/j.tetasy.2005.08.055
https://doi.org/10.1016/j.tetasy.2005.08.055
Publikováno v:
Angewandte Chemie International Edition. 44:3485-3488
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::183b392af7edd26500110b21f9c45e60
https://doi.org/10.1002/anie.200500564
https://doi.org/10.1002/anie.200500564
Publikováno v:
Advanced Synthesis & Catalysis. 346:359-366
Homobenzylic amides and carbamates, upon single-electron oxidation, undergo mesolytic cleavage reactions to form acyliminium ions. Appending nucleophilic groups to these substrates results in cyclization reactions to form N-acylaminals. The N-methylq
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0722871c9b037a86579ea1ab3fcca634
https://doi.org/10.1002/adsc.200303173
https://doi.org/10.1002/adsc.200303173