Search Results - "Belliotti, Thomas R."

Oxadiazolone bioisosteres of pregabalin and gabapentin by Wustrow, David J., Belliotti, Thomas R., Capiris, Thomas, Kneen, Clare O., Bryans, Justin S., Field, Mark J., Williams, Dic, El-Kattan, Ayman, Buchholz, Lisa, Kinsora, Jack J., Lotarski, Susan M., Vartanian, Mark G., Taylor, Charles P., Donevan, Sean D., Thorpe, Andrew J., Schwarz, Jacob B.

“…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…”
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Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones by Wagman, Allan S., Cirz, Ryan, McEnroe, Glenn, Aggen, James, Linsell, Martin S., Goldblum, Adam A., Lopez, Sara, Gomez, Marcela, Miller, George, Simons, Lloyd J., Belliotti, Thomas R., Harris, Christina R., Poel, Toni‐Jo, Melnick, Michael J., Gaston, Ricky D., Moser, Heinz E.

“…Conformationally constrained tetracyclic fluoroquinolones (FQs) were synthesized and profiled for their microbiological spectrum. The installation of a…”
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Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein by Belliotti, Thomas R, Capiris, Thomas, Ekhato, I. Victor, Kinsora, Jack J, Field, Mark J, Heffner, Thomas G, Meltzer, Leonard T, Schwarz, Jacob B, Taylor, Charles P, Thorpe, Andrew J, Vartanian, Mark G, Wise, Lawrence D, Zhi-Su, Ti, Weber, Mark L, Wustrow, David J

“…Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic, anxiolytic, and antihyperalgesic clinical efficacy. It binds…”
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Cover Feature: Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones (ChemMedChem 20/2017) by Wagman, Allan S., Cirz, Ryan, McEnroe, Glenn, Aggen, James, Linsell, Martin S., Goldblum, Adam A., Lopez, Sara, Gomez, Marcela, Miller, George, Simons, Lloyd J., Belliotti, Thomas R., Harris, Christina R., Poel, Toni‐Jo, Melnick, Michael J., Gaston, Ricky D., Moser, Heinz E.

“…The Cover Feature shows the conceptual conversion of clinafloxacin to its tetracyclic analog by addition of a 7‐membered ring, thereby conformationally fixing…”
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Isoindolinone enantiomers having affinity for the dopamine D4 receptor by BELLIOTTI, T. R, BRINK, W. A, WISE, L. D, KESTEN, S. R, RUBIN, J. R, WUSTROW, D. J, ZOSKI, K. T, WHETZEL, S. Z, CORBIN, A. E, PUGSLEY, T. A, HEFFNER, T. G

“…PD 108635 (1) was identified as a potent dopamine D4 ligand and we wanted to replace the benzylic alcohol with a metabolically more stable moiety…”
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A Series of 6- and 7-Piperazinyl- and -Piperidinylmethylbenzoxazinones with Dopamine D4 Antagonist Activity:  Discovery of a Potential Atypical Antipsychotic Agent by Belliotti, Thomas R, Wustrow, David J, Brink, Wouter A, Zoski, Kim T, Shih, Yu-Hsin, Whetzel, Steven Z, Georgic, Lynn M, Corbin, Ann E, Akunne, Hyacinth C, Heffner, Thomas G, Pugsley, Thomas A, Wise, Lawrence D

“…As part of a program to develop dopamine D4 antagonists for the treatment of schizophrenia, we discovered a series of 6- and 7-(phenylpiperazinyl)- and…”
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Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors by Flynn, Daniel L, Belliotti, Thomas R, Boctor, Amal M, Connor, David T, Kostlan, Catherine R, Nies, Donald E, Ortwine, Daniel F, Schrier, Denis J, Sircar, Jagadish C

“…A series of styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles were prepared and found to be dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat…”
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Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein by Belliotti, Thomas R, Capiris, Thomas, Ekhato, I Victor, Kinsora, Jack J, Field, Mark J, Heffner, Thomas G, Meltzer, Leonard T, Schwarz, Jacob B, Taylor, Charles P, Thorpe, Andrew J, Vartanian, Mark G, Wise, Lawrence D, Zhi-Su, Ti, Weber, Mark L, Wustrow, David J

“…Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic, anxiolytic, and antihyperalgesic clinical efficacy. It binds…”
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Isoindolinone enantiomers having affinity for the dopamine D 4 receptor by Belliotti, Thomas R., Brink, Wouter A., Kesten, Suzanne R., Rubin, John R., Wustrow, David J., Zoski, Kim T., Whetzel, Steven Z., Corbin, Ann E., Pugsley, Thomas A., Heffner, Thomas G., Wise, Lawrence D.

“…PD 108635 ( 1) was identified as a potent dopamine D 4 ligand and we wanted to replace the benzylic alcohol with a metabolically more stable moiety…”
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Structure−Activity Relationships of Pregabalin and Analogues That Target the α 2 -δ Protein by Belliotti, Thomas R., Capiris, Thomas, Ekhato, I. Victor, Kinsora, Jack J., Field, Mark J., Heffner, Thomas G., Meltzer, Leonard T., Schwarz, Jacob B., Taylor, Charles P., Thorpe, Andrew J., Vartanian, Mark G., Wise, Lawrence D., Zhi-Su, Ti, Weber, Mark L., Wustrow, David J.

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Novel cyclohexyl amides as potent and selective D 3 dopamine receptor ligands by Belliotti, Thomas R., Kesten, Suzanne R., Rubin, John R., Wustrow, David J., Georgic, Lynn M., Zoski, Kim T., Akunne, Hyacinth C., Wise, Lawrence D.

“…The dopamine D 3 receptor is an attractive target for the treatment of schizophrenia. We identified PD137557 ( V) as a ligand for the D 2 receptor and desired…”
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Novel cyclohexyl amides as potent and selective D3 dopamine receptor ligands by BELLIOTTI, T. R, KESTEN, S. R, RUBIN, J. R, WUSTROW, D. J, GEORGIC, L. M, ZOSKI, K. T, AKUNNE, H. C, WISE, L. D

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