Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Deborah A, Mischke"'
Autor:
Rhonda M Lachance, Stephen R. Rapp, John J. Parlow, Peter Harris, Rita M. Huff, Case Brenda, Mary W. Burney, Thomas J. Girard, Deborah A. Mischke, Ennis Michael D, Rhonda S. Woerndle, Kerri A. Hall, Ronald R. Hiebsch
Publikováno v:
Journal of Medicinal Chemistry. 53:2010-2037
Polymer-assisted solution-phase (PASP) parallel library synthesis was used to discover a piperazinyl glutamate pyridine as a P2Y(12) antagonist. Exploitation of this lead provided compounds with excellent inhibition of platelet aggregation as measure
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59f6174166fe97444d9135003e4fe44c
https://doi.org/10.1021/jm901518t
https://doi.org/10.1021/jm901518t
Autor:
John J, Parlow, Mary W, Burney, Brenda L, Case, Thomas J, Girard, Kerri A, Hall, Peter K, Harris, Ronald R, Hiebsch, Rita M, Huff, Rhonda M, Lachance, Deborah A, Mischke, Stephen R, Rapp, Rhonda S, Woerndle, Michael D, Ennis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1388-1394
Efforts to refine the SAR of the piperazinyl-glutamate-pyridines for more potent analogs with improved pharmacokinetic profiles are described. Exploring substituted piperidines and other ring systems at the 4-pyridyl position led to compounds with im
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffa8e3393275c3b43dc35183d05b48db
https://doi.org/10.1016/j.bmcl.2009.12.110
https://doi.org/10.1016/j.bmcl.2009.12.110
Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation
Autor:
Kerri A. Hall, Rita M. Huff, Rhonda M. Lachance, Ennis Michael D, Rhonda S. Woerndle, Ronald R. Hiebsch, John J. Parlow, Stephen R. Rapp, Deborah A. Mischke, Brenda L. Case, Mary W. Burney, Thomas J. Girard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6148-6156
Piperazinyl-glutamate-pyrimidines were prepared with oxygen, nitrogen, and sulfur substitution at the 4-position of the pyrimidine leading to highly potent P2Y 12 antagonists. In particular, 4-substituted piperidine-4-pyrimidines provided compounds w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da90bff048b77255c54d7a7a094fdeb9
https://doi.org/10.1016/j.bmcl.2009.09.017
https://doi.org/10.1016/j.bmcl.2009.09.017
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:
Michele A Melton, Nigam P. Rath, Ming Zeng, Margaret L. Grapperhaus, Brian S Hickory, Jane L Wang, Elaine S. Krul, Deborah M. Heuvelman, Mark E. Smith, Kevin C. Glenn, Richard C Durley, Deborah A. Mischke, Bryan J. Witherbee, Daniel T. Connolly, Dale P Spangler, Dorothy D. Honda, Yvette M. Fobian, James A. Sikorski, Mark A. Massa, Barry L. Parnas
Publikováno v:
Journal of Medicinal Chemistry. 45:3891-3904
A novel series of substituted N-benzyl-N-phenyl-trifluoro-3-amino-2-propanols are described that reversibly inhibit cholesteryl ester transfer protein (CETP). Starting with screening lead 22, various structural features were explored with respect to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::054e4cc40c00d2928100cc032ffe6208
https://doi.org/10.1021/jm020038h
https://doi.org/10.1021/jm020038h
Autor:
Deborah Aileen Mischke, Daniel M. Walker, Robert C. Chott, Kevin D. Jerome, Gopi Yalamanchili, Bruce Cameron Hamper
Publikováno v:
Biotechnology and Bioengineering. 71:28-37
Using a combination of solid phase synthesis for the preparation of N-substituted-N-acylglycines 7 followed by solution-phase ring transformation of trifluoromethylacyl munchnone intermediate 8, a library of 200 trisubstituted-5-trifluoromethylketo (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e221a08964e25f476e57c2c71fa8438b
https://doi.org/10.1002/(sici)1097-0290(200024)71:1<28::aid-bit5>3.0.co
https://doi.org/10.1002/(sici)1097-0290(200024)71:1<28::aid-bit5>3.0.co
Publikováno v:
The Journal of Organic Chemistry. 62:5908-5919
The use of our recently reported chemical library purification strategy in the development of a herbicidal lead, N-(3-benzoylphenyl)-3-(1,1-dimethylethyl)-1-methyl-1H-pyrazole-5-carboxamide (3), is described. The approach applying fundamental propert
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::87c87aa4911cdc1b043329dcd6e19b2e
https://doi.org/10.1021/jo970571i
https://doi.org/10.1021/jo970571i
Autor:
Peter Harris, Kerri A. Hall, Mary W. Burney, Thomas J. Girard, Stephen R. Rapp, Rita M. Huff, Ronald R. Hiebsch, Rhonda M Lachance, Case Brenda, Ennis Michael D, Rhonda S. Woerndle, Deborah A. Mischke, John J. Parlow
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
Polymer-assisted solution-phase (PASP) parallel library synthesis was used to discover a piperazinyl glutamate pyridine as a P2Y12 antagonist. Exploitation of this lead provided compounds with excellent inhibition of platelet aggregation as measured
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6af70aba9ebebe44b65412105d0dcebc
https://pubmed.ncbi.nlm.nih.gov/19604694
https://pubmed.ncbi.nlm.nih.gov/19604694
Autor:
Nigam P. Rath, Bryan J. Witherbee, Elaine S. Krul, Daniel T. Connolly, Deborah A. Mischke, Kevin C. Glenn, Ming Zeng, Richard C. Durley, Margaret L. Grapperhaus, Barry L. Parnas, Dorothy D. Honda, Mark E. Smith, Deborah M. Heuvelman, Yvette M. Fobian, James A. Sikorski, Mark A. Massa
Publikováno v:
Journal of medicinal chemistry. 43(24)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04770cfc11829c125c8f73a53ee361f1
https://pubmed.ncbi.nlm.nih.gov/11101348
https://pubmed.ncbi.nlm.nih.gov/11101348