Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Thomas Richard Belliotti"'
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:
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:
David Juergen Wustrow, Thomas G. Heffner, Michael Duff Davis, Lynn M. Georgic, Suzanne Ross Kesten, Anthony C. Blackburn, Ronald Rubin, Thomas Richard Belliotti, Shelly Ann Glase, Ann E. Corbin, Hyacinth Akunne, T. A. Pugsley, Norman L. Colbry, Steven Z. Whetzel, Kim Zoski, Lawrence D. Wise, D. R. Johnson
Publikováno v:
Journal of Medicinal Chemistry. 41:760-771
A series of [4-[2(4-arylpiperazin-1-yl)alkyl]cyclohexyl]pyrimidin-2-ylamine s was prepared and found to have receptor binding affinity for D2 and D3 dopamine (DA) receptors and serotonin 5-HT1A receptors. The structural contributions to D2/D3 and 5-H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a87db13947cb7fb22fb6f9cfb72e85f
https://doi.org/10.1021/jm9707378
https://doi.org/10.1021/jm9707378
Autor:
Thomas Richard Belliotti, J. R. Rubin, Lynn M. Georgic, David Juergen Wustrow, Lawrence D. Wise, Suzanne Ross Kesten, Kim T. Zoski, Hyacinth C. Akunne
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2403-2408
The dopamine D3 receptor is an attractive target for the treatment of schizophrenia. We identified PD137557 (V) as a ligand for the D2 receptor and desired to prepare a selective D3 compound. SAR studies involving different amides and different pheny
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c5f8c640079778ee6a291c1b3d9251e6
https://doi.org/10.1016/s0960-894x(97)00443-5
https://doi.org/10.1016/s0960-894x(97)00443-5
Autor:
Daniel L. Flynn, David T. Connor, Daniel F. Ortwine, Donald E. Nies, Amal M. Boctor, Catherine R. Kostlan, Denis J. Schrier, Thomas Richard Belliotti, Jagadish C. Sircar
Publikováno v:
ChemInform. 22
A series of styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles were prepared and found to be dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia cells. Compounds from this series also were found to inhibit the in vi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::733ae2d1e12df54a5c8c6f54c5b93744
https://doi.org/10.1002/chin.199138154
https://doi.org/10.1002/chin.199138154
Autor:
J. R. Rubin, David Juergen Wustrow, Lynn M. Georgic, Suzanne Ross Kesten, Thomas Richard Belliotti, Hyacinth C. Akunne, Lawrence D. Wise, Kim T. Zoski
Publikováno v:
ChemInform. 29
The dopamine D3 receptor is an attractive target for the treatment of schizophrenia. We identified PD137557 (V) as a ligand for the D2 receptor and desired to prepare a selective D3 compound. SAR studies involving different amides and different pheny
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::23b4044d0797d80f2431438cb02dacd2
https://doi.org/10.1002/chin.199804150
https://doi.org/10.1002/chin.199804150
Publikováno v:
ChemInform. 29
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c0a5bf39a9175a4889568be6ca5edbb6
https://doi.org/10.1002/chin.199841154
https://doi.org/10.1002/chin.199841154
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:
Jeremy J. Edmunds, Suzie Ferreira, Mehran Jalaie, Rajendra Subedi, Daniel D. Holsworth, Erli Zhang, Samarendra N. Maiti, Patrick I. McConnell, John W. Bryant, Tingsheng Li, Noel A. Powell, Thomas Richard Belliotti, Cuiman Cai, Michael J. Ryan, Igor Mochalkin, Michael Stier, Aparna Kasani, Wendy Collard
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(13)
Novel 2,4-diaminopyrimidine-based small molecule renin inhibitors are disclosed. Through high throughput screening, parallel synthesis, X-ray crystallography, and structure based drug design, we have developed the first non-chiral, non-peptidic, smal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f35fd8fc9154831be467ecd329f62af
https://pubmed.ncbi.nlm.nih.gov/17482464
https://pubmed.ncbi.nlm.nih.gov/17482464