Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Thomas Capiris"'
Autor:
Howard Roark, Matthew Robert Johnson, Michael Stier, Thomas Capiris, Peter R. Guzzo, Thomas Richard Belliotti, John E. Mangette, Van-Duc Le, Rajesh A. Shenoy
Publikováno v:
Tetrahedron. 65:9536-9541
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::60462e0a85f98e758d1a19953a84e275
https://doi.org/10.1016/j.tet.2009.09.045
https://doi.org/10.1016/j.tet.2009.09.045
Autor:
Jack J. Kinsora, N. Suman-Chauhan, Clare O. Kneen, Karen Walters, Cindy M. Donovan, David J. Wustrow, Thomas Capiris, David J. Dooley, Ayman El-Kattan, Mark G. Vartanian, Lisa R. Thompson, Susan M. Lotarski, Simon A. Osborne, Jacob Bradley Schwarz, Mark J. Field, Carmen E. Burgos-Lepley, Charles Taylor, Justin Stephen Bryans, Madhu Cherukury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2333-2336
A series of carboxylate bioisosteres of structures related to gabapentin 1 have been prepared. When the carboxylate was replaced by a tetrazole, this group was recognized by the alpha2-delta protein. Further characterization of alpha2-delta binding c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15c268505093a43a39031f57a037129d
https://doi.org/10.1016/j.bmcl.2005.05.016
https://doi.org/10.1016/j.bmcl.2005.05.016
Autor:
Thomas G. Heffner, Jack J. Kinsora, Jacob Bradley Schwarz, Ti Zhi-Su, David J. Wustrow, Leonard T. Meltzer, Thomas Richard Belliotti, Thomas Capiris, Andrew John Thorpe, Lawrence D. Wise, Mark L. Weber, Charles Taylor, Mark J. Field, Mark G. Vartanian, I.Victor Ekhato
Publikováno v:
Journal of Medicinal Chemistry. 48:2294-2307
Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic, anxiolytic, and antihyperalgesic clinical efficacy. It binds with high affinity to the alpha(2)-delta subunit of voltage-gated calcium channels and is a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c05d681e9f725c4f7d0de7f09212832b
https://doi.org/10.1021/jm049762l
https://doi.org/10.1021/jm049762l
Autor:
Robert G. MacKenzie, Ronald Rubin, Thomas Capiris, Thomas G. Heffner, M. Duff Davis, Kim Zoski, Hyacinth Akunne, Lawrence D. Wise, T. A. Pugsley, James A. Knobelsdorf, David J. Wustrow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2067-2070
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and sugges
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9a93668170624fa56fe27b8bafacae7
https://doi.org/10.1016/s0960-894x(98)00372-2
https://doi.org/10.1016/s0960-894x(98)00372-2
Autor:
David T. Connor, Robert Doubleday, Lawrence D. Wise, Robert G. MacKenzie, Thomas Capiris, Thomas G. Heffner, Steven Robert Miller, Thomas A. Pugsley, Paul C. Unangst
Publikováno v:
Journal of Medicinal Chemistry. 40:4026-4029
The discovery of a series of novel (aryloxy)alkylamines with selective affinity for the dopamine D4 receptor is described. Target compounds were tested for binding to cloned human dopamine D2, D3, and D4 receptor subtypes expressed in Chinese hamster
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a58a8a70268dfe3365f29e9f5a83a4d
https://doi.org/10.1021/jm970422s
https://doi.org/10.1021/jm970422s
Autor:
Steven Robert Miller, David T. Connor, Lawrence D. Wise, Robert G. MacKenzie, Thomas G. Heffner, and Thomas A. Pugsley, Thomas Capiris, Paul C. Unangst
Publikováno v:
Journal of Medicinal Chemistry. 40:2688-2693
The discovery of a series of chromeno[3,4-c]pyridin-5-ones with selective affinity for the dopamine D4 receptor is described. Target compounds were tested for binding to cloned human dopamine D2, D3, and D4 receptor subtypes expressed in Chinese hams
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b95a99c1a2a18124a0b2b93804ca6180
https://doi.org/10.1021/jm970170v
https://doi.org/10.1021/jm970170v
Autor:
Dirk A. Bornemeier, David T. Connor, Paul J. Kuipers, Diane H. Boschelli, Jagadish C. Sircar, Clifford D. Wright, Mark E. Lesch, Denis J. Schrier, Thomas Capiris, James B. Kramer, G. C. N. Okonkwo, Richard D. Dyer, John A. Kennedy
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:403-410
The preparation of hydroxylamine analogs of 2,6-di-tert-butylphenols (DTBP) and the inhibition of cyclooxygenase (CO) and 5-lipoxygenase (5-LO) by these compounds is discussed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b8fa689d0631ac962855f6386d904d9
https://doi.org/10.1016/0968-0896(95)00027-e
https://doi.org/10.1016/0968-0896(95)00027-e
Autor:
Thomas Richard Belliotti, Rajesh A. Shenoy, Howard Roark, Van-Duc Le, Thomas Capiris, John E. Mangette, Peter R. Guzzo, Michael Stier, Matthew Robert Johnson
Publikováno v:
ChemInform. 41
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d678f825bdf7142cd79033e18ce8e3ba
https://doi.org/10.1002/chin.201010134
https://doi.org/10.1002/chin.201010134
Autor:
Thomas Richard Belliotti, Susan M. Lotarski, Justin Stephen Bryans, Dic Williams, Jack J. Kinsora, Clare O. Kneen, Andrew John Thorpe, David J. Wustrow, Jacob Bradley Schwarz, Ayman El-Kattan, Charles Taylor, Sean D. Donevan, Lisa Buchholz, Thomas Capiris, Mark G. Vartanian, Mark J. Field
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(1)
A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the α 2 -δ subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain uptak
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88d9b90cc172e35df292897ac3bce3f6
https://pubmed.ncbi.nlm.nih.gov/19010672
https://pubmed.ncbi.nlm.nih.gov/19010672
Autor:
Jagadish C. Sircar, Richard D. Dyer, Denis J. Schrier, David T. Connor, W. J. Cetenko, Donald E. Nies, C. R. Kostlan, Daniel L. Flynn, Thomas Capiris
Publikováno v:
Journal of Medicinal Chemistry. 33:2070-2072
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b32056e952e5b93824353c3034265cc3
https://doi.org/10.1021/jm00170a004
https://doi.org/10.1021/jm00170a004