Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Richard V. Trilles"'
Autor:
Julie Wilmowski, Hua Gao, Jana Polivkova, Dilinie P. Fernando, John R. Hadcock, Lucinda Thiede, Yue Chen, Angel Guzman-Perez, Paul Da Silva Jardine, Dennis O. Scott, Yingxin Zhang, Lucy Rogers, David Austen Perry, Denise Gautreau, Elena E. Beretta, Sophie Y. Lavergne, Catherine E. Trebino, Swick Andrew Gordon, Kimberly O. Cameron, Jeffrey T. Kohrt, Margaret Y. Chu-Moyer, Richard V. Trilles, Christopher F. Hoth, Sylvie Perez, Michael Raymond Makowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2943-2947
New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::545aee7651b73b6139e0a02a9907e42e
https://doi.org/10.1016/j.bmcl.2012.02.049
https://doi.org/10.1016/j.bmcl.2012.02.049
Autor:
Michael Raymond Makowski, David W. Piotrowski, Judith M. Cosgrove, John Litchfield, Claire M. Steppan, Janice A. Brown, Constantin Neagu, Yue Chen, Ping Du, David Austen Perry, Kelly A. Martin, Thomas J. McLellan, Richard V. Trilles, Karen Atkinson, Mayda Castrodad, Elena E. Beretta
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1621-1625
A potent, small molecule inhibitor with a favorable pharmacokinetic profile to allow for sustained SCD inhibition in vivo was identified. Starting from a low MW acyl guanidine (5a), identified with a RapidFire High-Throughput Mass Spectrometry (RF-MS
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7fc68ce50aec716130464effe4b0fa70
https://doi.org/10.1016/j.bmcl.2011.01.113
https://doi.org/10.1016/j.bmcl.2011.01.113
Autor:
Karen Rowan, Jefferson Wright Tilley, Richard V. Trilles, Dorota Miklowski, Virginia Schwinge, Li Chen, Tai-Nan Huang, Robert M. Campbell, David C. Fry
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1679-1682
A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afd7d731fdb244de48ba4c2810efc9ab
https://doi.org/10.1016/s0960-894x(02)00201-9
https://doi.org/10.1016/s0960-894x(02)00201-9
Autor:
Li Chen, Weiya Yun, Richard V. Trilles, Karen Rowan, David C. Fry, Jefferson Wright Tilley, Charles H. Cook, Virginia Schwinge, Robert M. Campbell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:137-140
A series of N-benzylpyroglutamyl-L-phenylalanine derivatives bearing carbamoyl substituents in the 3- or 4-positions was prepared and assayed for inhibition of the interaction between VCAM and VLA-4. Potent inhibition was observed in a number of anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e28b1c8519567294c5c8237e485742d
https://doi.org/10.1016/s0960-894x(01)00711-9
https://doi.org/10.1016/s0960-894x(01)00711-9
Autor:
Dorota Miklowski, Richard V. Trilles, Robert William Guthrie, Karen Rowan, Gerry Kaplan, Nicolas Huby, Barry A. Wolitzky, Jefferson Wright Tilley, Virginia Schwinge, Francis A. Mennona, Tai-Nan Huang, Li Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:729-733
A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d9701ff0e4ce4f658c7cfcb49aaa55f
https://doi.org/10.1016/s0960-894x(00)00089-5
https://doi.org/10.1016/s0960-894x(00)00089-5
Publikováno v:
Tetrahedron Letters. 36:8715-8718
Synthesis of an orthogonally protected form of phenylogous amino acid 1 which mimics an extended conformation of the dipeptide Arg-Gly was achieved. Key steps Involve a diastereoselective addition of allylic organomelallic reagenlS to chira! imine 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4618ced595f3259c5936b5a760bac437
https://doi.org/10.1016/0040-4039(95)01877-k
https://doi.org/10.1016/0040-4039(95)01877-k
Publikováno v:
ChemInform. 25
Efficient chain extension of β-D-galactopyranosyl cyanide, cyclization to a bicyclic octose, and then attachment of cytosine affords the ezomycin octosyl nucleoside 17 in a form suitable for elaboration to the ezomycins (e.g., 1)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d58c83c01523bea6640c2c694b4f0012
https://doi.org/10.1002/chin.199432231
https://doi.org/10.1002/chin.199432231
Publikováno v:
ChemInform. 27
Synthesis of an orthogonally protected form of phenylogous amino acid 1 which mimics an extended conformation of the dipeptide Arg-Gly was achieved. Key steps Involve a diastereoselective addition of allylic organomelallic reagenlS to chira! imine 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0ff8bdf5bb11e84d5947a9eb7e4af1d9
https://doi.org/10.1002/chin.199612226
https://doi.org/10.1002/chin.199612226
Autor:
Richard V. Trilles, David C. Fry, Virginia Schwinge, Weiya Yun, Robert M. Campbell, Karen Rowan, Li Chen, Charles H. Cook, Jefferson Wright Tilley
Publikováno v:
ChemInform. 33
A series of N-benzylpyroglutamyl-L-phenylalanine derivatives bearing carbamoyl substituents in the 3- or 4-positions was prepared and assayed for inhibition of the interaction between VCAM and VLA-4. Potent inhibition was observed in a number of anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b6227c1cfc9d5e9c0042ad46a477247b
https://doi.org/10.1002/chin.200219183
https://doi.org/10.1002/chin.200219183
Publikováno v:
ChemInform. 34
A three-step, readily scalable route for the conversion of a ring-conjugated tetrahydro-3H-phenanthren-2-one to a trans-fused hexahydro-1H-phenanthren-2-one is described. The key step is the hydrogenation of a double bond using a nearby ketal moiety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4225cfaeaf8486cc21c28dde2fba92b0
https://doi.org/10.1002/chin.200333186
https://doi.org/10.1002/chin.200333186