Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Bernard R. Neustadt"'
Autor:
Charles Lee Jayne, Hong Liu, Yan Xia, Santhosh Neelamkavil, William J. Greenlee, Hana Baker, Brian Hawes, Kim O’Neill, Andrew Stamford, Timothy J. Kowalski, Xing Dai, Jinsong Hao, Samuel Chackalamannil, Huadong Tang, Dipshikha Biswas, Bernard R. Neustadt, Craig D. Boyle
Publikováno v:
ACS Medicinal Chemistry Letters. 9:457-461
[Image: see text] The ever-growing prevalence of type 2 diabetes in the world has necessitated an urgent need for multiple orally effective agents that can regulate glucose homeostasis with a concurrent reduction in body weight. G-Protein coupled rec
Autor:
Abdallah Hadj-Tahar, Robert A. Hodgson, Thérèse Di Paolo, Tatiana M. Kazdoba, Andrew Stamford, Paul J. Bédard, Annamarie Pond, Aurelie Dare, Laurent Grégoire, John C. Hunter, Geoffrey B. Varty, Michael Grzelak, Bernard R. Neustadt, Nancy Bélanger
Publikováno v:
Experimental Neurology. 225:384-390
Parkinson's Disease (PD) and Extrapyramidal Syndrome (EPS) are movement disorders that result from degeneration of the dopaminergic input to the striatum and chronic inhibition of striatal dopamine D(2) receptors by antipsychotics, respectively. Aden
Autor:
Leyla Arik, Geoffrey B. Varty, Hongtao Zhang, Jean E. Lachowicz, Bernard R. Neustadt, Rosalia Bertorelli, Hong Liu, William J. Greenlee, Andrew Stamford, Mary Cohen-Williams, Silva Fredduzzi, Carolyn Foster, Jinsong Hao, Kwokei Ng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:967-971
Antagonism of the adenosine A(2a) receptor offers great promise in the treatment of Parkinson's disease. In the course of exploring pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, which led to clinical candidate SCH 420814, we prep
Autor:
Samuel Chackalamannil, Shiyong Wang, Leyla Arik, Craig D. Boyle, Carolyn Foster, Ying Zhai, Lindo Neil A, Kwokei Ng, Bernard R. Neustadt, Angela Monopoli, Unmesh Shah, William J. Greenlee, Jean E. Lachowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4199-4203
SCH 58261 is a reported adenosine A2A receptor antagonist, which is active in rat in vivo models of Parkinson’s Disease upon ip administration. However, it has poor selectivity versus the A1 receptor and does not demonstrate oral activity. We repor
Autor:
Claire M. Lankin, Geoffrey B. Varty, Samuel Chackalamannil, William J. Greenlee, Kwokei Ng, Guy A. Higgins, Mary Cohen-Williams, Craig D. Boyle, Unmesh Shah, Jean E. Lachowicz, Hongtao Zhang, Bernard R. Neustadt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4204-4209
SCH 58261 is a reported adenosine A(2A) receptor antagonist which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A(1) receptor and does not demonstrate oral activity. Quinoli
Autor:
Andrew Stamford, Bernard R. Neustadt, Lindo Neil A, Deen Tulshian, Kwokei Ng, Carolyn Foster, William J. Greenlee, Ennio Ongini, Jean E. Lachowicz, John C. Hunter, Jinsong Hao, Kung-I Feng, Rosalia Bertorelli, Leyla Arik, Angela Monopoli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1376-1380
Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonist SCH 58261 as a starting point, we identified the potent and sele
Autor:
Xiaoying Xu, Timothy J. Kowalski, William J. Greenlee, Hong Liu, Andrew Stamford, Brian Hawes, Xing Dai, Morgan Woods, Huadong Tang, Bernard R. Neustadt, Kim O’Neill, Hana Baker, Jingsong Hao
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(22)
The design and synthesis of two conformationally restricted oxazabicyclo octane derivatives as GRP119 agonists is described. Derivatives of scaffold C, with syn configuration, have the best overall profiles with respect to solubility and in vivo effi
Autor:
Deen Tulshian, Carolyn Foster, Julius J. Matasi, Jinsong Hao, Bernard R. Neustadt, Leyla Arik, Jean E. Lachowicz, John P. Caldwell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1333-1336
In high throughput screening of our file compounds, a novel structure 1 was identified as a potent A(2A) receptor antagonist with no selectivity over the A1 adenosine receptor. The structure-activity relationship investigation using 1 as a template l
Autor:
Michael G. Murray, Bernard R. Neustadt, Julie M. Strizki, Sue-Ing Lin, Nicole Vantuno, Lisa Wojcik, Jayaram R. Tagat, Kathleen Cox, and Bahige M. Baroudy, Steensma Ruo, Dennis V. Nazareno, Stuart W. McCombie, Serena Xu
Publikováno v:
Journal of Medicinal Chemistry. 44:3343-3346
Truncation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. Further optimization for
Publikováno v:
Tetrahedron Letters. 39:5317-5320
A convenient large-scale preparation of the trifunctional acid 1 has been developed. This acid serves as a useful scaffold for construction of combinatorial libraries incorporating three variable elements in a centro-symmetric array.