Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Michael B, Tollefson"'
Autor:
Robert Hughes, Michael B. Tollefson, Michael John Palmer, Brad A. Acker, Brian R. Bond, Fox David Nathan Abraham, Ying Yu, E. J. Jacobsen, John K. Walker, Sandra K. Freeman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3120-3124
1H-Pyrazolo[4,3-d]pyrimidines are a class of potent and selective second generation phosphodiesterase 5 (PDE5) inhibitors. This work explores the potency, selectivity and efficacy of 1-(2-ethoxyethyl)-1H-pyrazolo[4,5-d]pyrimidines as PDE5 inhibitors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::237d1b41e2f31e4be9891479b99bb481
https://doi.org/10.1016/j.bmcl.2010.03.111
https://doi.org/10.1016/j.bmcl.2010.03.111
Autor:
Brian R. Bond, Michael John Palmer, John K. Walker, Ying Yu, Michael B. Tollefson, Brad A. Acker, Fox David Nathan Abraham, Sandra K. Freeman, Eric Jon Jacobsen, Robert Hughes
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3125-3128
1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the substitution of 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23c9d94689adec47a050353153ec9f14
https://doi.org/10.1016/j.bmcl.2010.03.106
https://doi.org/10.1016/j.bmcl.2010.03.106
Autor:
Maddux Todd Michael, Yvette M. Fobian, Alan G. Benson, Dafydd R. Owen, Brian R. Bond, Christopher Phillips, Brad A. Acker, E. Jon Jacobsen, Michael John Palmer, D. Joseph Rogier, John M. Molyneaux, Brent V. Mischke, John N. Freskos, Tracy J. Ringer, Andrew Simon Bell, Blevis-Bal Radhika M, Robert Hughes, David G. Brown, Steve E. Heasley, Joseph B. Moon, John K. Walker, Brown David L, William C. Stallings, Michael B. Tollefson, Alan MacInnes, Jerry W. Cubbage, Yung Yu, Margarita Rodriquez-Lens, Fox David Nathan Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4088-4091
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5005db6742e606fdadbf520ea66a63a9
https://doi.org/10.1016/j.bmcl.2009.06.012
https://doi.org/10.1016/j.bmcl.2009.06.012
Autor:
Christopher R. Dalton, Nizal S. Chandrakumar, Mark L. Boys, G. Allen Nickols, Mark Russell, Maureen A. Nickols, Michael Clare, Dale P. Spangler, John A. Wendt, Christina N. Steininger, William F. Westlin, Yaping Wang, Tiffany Duffin, Michael B. Tollefson, Jon A. Klover, Sandra K. Freeman, Melanie L. Hanneke, Scott B. Mohler, Mary Beth Finn, Maria N. Nguyen, Heather G. Stenmark, Jeffery L. Keene, Hongwei Wu, Bipin N. Desai, Barbara B. Chen, V. Wayne Engleman, Yi X. Yu, Sarah A. Norring, Marisa M. Westlin, Lori A. Schretzman, Downs Victoria Leigh, Ish K. Khanna, Thomas D. Penning
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:839-844
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::701f9513e934e8bf576a289475c31d0e
https://doi.org/10.1016/j.bmcl.2005.11.008
https://doi.org/10.1016/j.bmcl.2005.11.008
Discovery of Potent, Nonsystemic Apical Sodium-Codependent Bile Acid Transporter Inhibitors (Part 2)
Autor:
Miller Raymond E, Wei Huang, Horng-Chih Huang, Jay S. Trivedi, Scott R. Both, Nigam P. Rath, David B. Reitz, Deborah A. Mischke, Len F. Lee, Samuel J. Tremont, Steve R. Rapp, Danny J. Garland, Claude Jones, Banerjee Shyamal C, Matthew W. Mahoney, Theresa Fletcher, Michael B. Tollefson, Karen Regina, Emily J. Reinhard, Grace M. Wagner, Mark E. Smith, Judy Beaudry, J.-H Li, Kevin C. Glenn, Bradley T. Keller, Robert E. Manning, Kevin J. Koeller, Joe R. Schuh, Kolodziej Steve A, William F. Vernier, Carpenter Andrew J, Ching-Cheng Wang
Publikováno v:
Journal of Medicinal Chemistry. 48:5853-5868
In the preceding paper several compounds were reported as potent apical sodium-codependent bile acid transporter (ASBT) inhibitors. Since the primary site for active bile acid reabsorption is via ASBT, which is localized on the luminal surface of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8126ad3914a164ee565779032f3a9bd
https://doi.org/10.1021/jm0402162
https://doi.org/10.1021/jm0402162
Discovery of Potent, Nonsystemic Apical Sodium-Codependent Bile Acid Transporter Inhibitors (Part 1)
Autor:
Len F. Lee, James C. B. Li, William F. Vernier, Samuel J. Tremont, Miller Raymond E, Claude Jones, Wei Huang, Kevin J. Koeller, Robert E. Manning, Andrew J. Carpenter, Mark E. Smith, Scott R. Both, Nigam P. Rath, Joe R. Schuh, Michael B. Tollefson, Jay S. Trivedi, Danny J. Garland, Emily J. Reinhard, Deborah A. Mischke, Karen Regina, David B. Reitz, Grace M. Wagner, Ching-Cheng Wang, Kolodziej Steve A, Kevin C. Glenn, Keller Bradley T, Steve R. Rapp, Banerjee Shyamal C, Theresa R. Fletcher, Horng-Chih Huang, Judy Beaudry, Matthew W. Mahoney
Publikováno v:
Journal of Medicinal Chemistry. 48:5837-5852
Elevated plasma levels of low-density lipoprotein (LDL) cholesterol are a major risk factor for atherosclerosis leading to coronary artery disease (CAD), which remains the main cause of mortality in Western society. We believe that by preventing the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0eb4d79f2a819622faa896314c94f38
https://doi.org/10.1021/jm040215+
https://doi.org/10.1021/jm040215+
Autor:
Sheri L. Bonar, Adam Libby, Yao Min, Richard Weier, Michael B. Tollefson, Serge G. Wolfson, Michael Clare, Ann M. Donnelly, William E. Mcghee, Dominique Bonafoux, Patrick J. Lennon, Sumathy Mathialagan, Julia A. Guzova, Nandini Kishore, Cindy Sommers, Sharon Rouw, Lori Christine, Catherine S. Tripp
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2870-2875
A series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2. In spite of their often modest activity on the enzyme, six selected analogs showed significant inhibition o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::752b9930690fa8fa16c025496d6ce863
https://doi.org/10.1016/j.bmcl.2005.03.090
https://doi.org/10.1016/j.bmcl.2005.03.090
Autor:
Jane L. Wang, Michael B. Tollefson, Margaret L. Grapperhaus, James A. Sikorski, Richard C. Durley, Monica B. Norton, Michele A. Promo, Michele A. Melton, Mark A. Massa, Emily J. Reinhard, Brian S. Hickory, William F. Vernier, Mark E. Smith, Yvette M. Fobian, Karen Regina, Bryan J. Witherbee, Daniel T. Connolly
Publikováno v:
Journal of Medicinal Chemistry. 46:2152-2168
A novel series of substituted N-[3-(1,1,2,2-tetrafluoroethoxy)benzyl]-N-(3-phenoxyphenyl)-trifluoro-3-amino-2-propanols is described which potently and reversibly inhibit cholesteryl ester transfer protein (CETP). Starting from the initial lead 1, va
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b10e457203bbb1110208e3911dfa6aac
https://doi.org/10.1021/jm020528+
https://doi.org/10.1021/jm020528+
Publikováno v:
Journal of the American Chemical Society. 118:9052-9061
Double labeling has been used under the endocyclic restriction test to show that transfers of phosphorus from oxygen to carbon in the conversions of lithio phosphinite 1 to alkoxy phosphine 8, of lithio phosphinite 2 to alkoxy phosphine 9, of lithio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2df243969ea9069ec68242ef033b9e71
https://doi.org/10.1021/ja961375g
https://doi.org/10.1021/ja961375g
Publikováno v:
Journal of the American Chemical Society. 115:6548-6556
The equation of which stage of the triplet di-r-methane rearrangement controls the regiochemistry and excited-state rate was resolved in the present investigation. In this study, using m-cyanodibenzobarrelene, the m-cyano substituent was located in a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6a0bca6fa7f11c6efba0de953ed9ad92
https://doi.org/10.1021/ja00068a011
https://doi.org/10.1021/ja00068a011