Zobrazeno 1 - 10
of 59
pro vyhledávání: '"David B. Reitz"'
Autor:
Danny J. Garland, Wei Huang, Michael S. South, Matthew W. Mahoney, Zaheer Abbas, David B. Reitz, John I. Trujillo, William L. Neumann, Carrie L. Kusturin, Horng-Chih Huang, Scott A. Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4568-4574
Herein is described the design, synthesis, and enzymatic activity of a series of substituted pyrazinones as inhibitors of the TF/VIIa complex. These inhibitors were designed to explore replacement and variation of the P1 amidine described previously
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::871460a02f00bed63c759ec3cd4efa14
https://doi.org/10.1016/j.bmcl.2007.05.090
https://doi.org/10.1016/j.bmcl.2007.05.090
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+
Publikováno v:
Organic Preparations and Procedures International. 34:271-319
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3d4402e9f0e175ef3ac3330fb53cf566
https://doi.org/10.1080/00304940209356771
https://doi.org/10.1080/00304940209356771
Publikováno v:
The Journal of Organic Chemistry. 65:2711-2715
A highly enantioselective synthesis of benzothiepine 1a has been accomplished via an enantioenriched sulfoxide intermediate obtained by asymmetric oxidation with a chiral oxaziridine in 89:11 er. The key step is a thermodynamically controlled asymmet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98967fad701251e3aa347c0250574edb
https://doi.org/10.1021/jo991786q
https://doi.org/10.1021/jo991786q
Autor:
Gary D. Anderson, A. W. Veenhuizen, Carol M. Koboldt, Karen Seibert, Robert E. Manning, William E. Perkins, Yan Zhang, Horng-Chi Huang, J. N. Cogburn, D. J. Garland, Jinglin Li, Emily J. Reinhard, David B. Reitz, S. A. Gregory, Timothy S. Chamberlain, E. G. Burton, Peter C. Isakson
Publikováno v:
Journal of Medicinal Chemistry. 39:253-266
A novel series of 5,6-diarylspiro[2.4]hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3,4-disubstituted phenyl analogs are gene
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c9ef2e75bc7cbe29bd4ca9744f026f5
https://doi.org/10.1021/jm950664x
https://doi.org/10.1021/jm950664x
Novel Terphenyls as Selective Cyclooxygenase-2 Inhibitors and Orally Active Anti-inflammatory Agents
Autor:
Peter C. Isakson, James J. Li, David B. Reitz, G. D. Anderson, Monica B. Norton, Carol M. Koboldt, Jaime L. Masferrer, Gregory Susan A, Emily J. Reinhard, Karen Seibert, Yan Zhang, Ben S. Zweifel, William Perkins
Publikováno v:
Journal of Medicinal Chemistry. 39:1846-1856
A novel series of terphenyl methyl sulfones and sulfonamides have been shown to be highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. The sulfonamide analogs 17 and 21 were found to be much more potent COX-2 inhibitors and orally active
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2a6917aad0904e60acdaab0eb7bd0ed
https://doi.org/10.1021/jm950878e
https://doi.org/10.1021/jm950878e
Autor:
Karen Selbert, Timothy S. Chamberlain, David B. Reitz, Carol M. Koboldt, Horng-Chih Huang, Peter C. Isakson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2377-2380
Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. A structure-activity relationship study suggests that the conversion of sulfones to sulfonamides affords potent, but slightly less selective C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::aa255af019c02cd704540e412b74ec35
https://doi.org/10.1016/0960-894x(95)00414-o
https://doi.org/10.1016/0960-894x(95)00414-o
Autor:
David B. Reitz, Peter C. Isakson
Publikováno v:
Current Pharmaceutical Design. 1:211-220
Prostaglandins are synthesized by the enzyme cyclooxygenase (COX), which is the target for nonsteroidal anti-inflammatory drugs (NSAIDs). Recently a second form of COX was discovered (COX-2) that is induced by inflammatory stimuli. The identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::57b66cd9d1f72624b0ff457a1308dc9b
https://doi.org/10.2174/1381612801666220917221427
https://doi.org/10.2174/1381612801666220917221427
Autor:
Karen Seibert, James J. Li, G. D. Anderson, Robert E. Manning, Carol M. Koboldt, Gregory Susan A, William Perkins, H.‐C. Huang, Danny J. Garland, David B. Reitz, Peter C. Isakson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:867-872
Novel 4,5-diarylspiro[2.4]hept-5-enes, 6,7-diarylspiro[3.4]oct-6-enes, and 2,3-diarylspiro[4.4]non-2-enes have been synthesized and shown to be very potent inducible cyclooxygenase (COX-2) inhibitors with inhibition (IC 50 ) in the low nanomolar rang
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fc0cc1a13c6b5960f6396e7c6d8c6a06
https://doi.org/10.1016/0960-894x(95)00131-c
https://doi.org/10.1016/0960-894x(95)00131-c