Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Manisha Moorjani"'
Autor:
Marion Lanier, Xiaohu Zhang, John E. Tellew, Zhiyong Luo, Mark Santos, Raymond S. Gross, Deborah H. Slee, Emily Lin, Sandra M. Lechner, Jaimie K. Rueter, María I. Crespo, Jose-Luis Diaz, Yongsheng Chen, Siobhan Malany, Manisha Moorjani, John Saunders, John P. Williams, Binh G. Vong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5402-5405
In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In additi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::799d40e0876b3b15e810f1648d5b9dc2
https://doi.org/10.1016/j.bmcl.2008.09.048
https://doi.org/10.1016/j.bmcl.2008.09.048
Autor:
Yongsheng Chen, Mark Santos, Emily Lin, Stacy Markison, John E. Tellew, Sandra M. Lechner, Maria Prat, Xiaohu Zhang, John Saunders, Silvia Gual, Marion Lanier, Marı´a I. Crespo, John P. Williams, Raymond S. Gross, Tanya Joswig, Jaimie K. Rueter, Deborah H. Slee, Siobhan Malany, Jose-Luis Diaz, Manisha Moorjani, Julio C. Castro-Palomino
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1778-1783
A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM), selectivity (A(1)/A(2A) > 100), and efficacy (MED 10 mg/kg p.o.) in the rat haloperidol-indu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26dca2261358c58ec30c26ccccacb9f1
https://doi.org/10.1016/j.bmcl.2008.02.032
https://doi.org/10.1016/j.bmcl.2008.02.032
Autor:
Charles Q. Huang, James R. McCarthy, Paul D. Crowe, Raymond S. Gross, John Saunders, Dimitri E. Grigoriadis, Jodene Nelson, Richard Lowe, Brian Dyck, John P. Williams, Dragan Marinkovic, Sam R. J. Hoare, Tim Coon, Robert W. Sullivan, Mustapha Haddach, Said Zamani-Kord, Manisha Moorjani, Zhiqiang Guo, Jane Han Bu, Takung Chen
Publikováno v:
Journal of Medicinal Chemistry. 48:5780-5793
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide should prove to be effective in treating stress and anxiety-related disorders. In an effort to identify antagonists with improved physicochemical properties, new tricyclic CRF(1) an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ed6584cab9355c213297346348adfa0
https://doi.org/10.1021/jm049085v
https://doi.org/10.1021/jm049085v
Autor:
Said Zamani-Kord, Brian Dyck, Zhiqiang Guo, Robert W. Sullivan, Zhiyong Luo, Raymond S. Gross, Manisha Moorjani, Bin-Feng Li, Mustapha Haddach, John E. Tellew, Mehrak Kiankarimi, Marion Lanier, John P. Williams, James R. McCarthy, Dimitri Grigoriadis, Ta Kung Chen, Paul D. Crowe, John Saunders, Xiaohu Zhang, Jonathan Grey
Publikováno v:
Journal of Medicinal Chemistry. 48:5104-5107
The synthesis and SAR studies of tricyclic imidazo[4,5-b]pyridin-2-ones as human corticotropin-releasing factor receptor (CRF(1)) antagonists are discussed herein. Compound 16g was identified as a functional antagonist that inhibited CRF-stimulated c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::815355c45c4d5367cde1ab00c4dece95
https://doi.org/10.1021/jm050384+
https://doi.org/10.1021/jm050384+
Autor:
Lee Carter, Oscar Acevedo, Susan K. Sullivan, Yun-Fei Zhu, Patrick J. Connors, John Saunders, Qiu Xie, Andrew Fisher, Chen Chen, Zhiqiang Guo, R. Scott Struthers, Manisha Moorjani, Martin W. Rowbottom, Fabio C. Tucci, Timothy D. Gross
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4967-4973
The synthesis of a series of ( R )-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5 is described. SAR around C-5 of the uracil led to the discovery that a 2-thienyl or (2-phenyl)thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afab3c785ff0457b782440bfeb65d930
https://doi.org/10.1016/j.bmcl.2004.07.022
https://doi.org/10.1016/j.bmcl.2004.07.022
Autor:
Emily Lin, Zhiyong Luo, Dimitri E. Grigoriadis, Marion Lanier, Xiaohu Zhang, Romano Di Fabio, Yves St. Denis, John E. Tellew, Enza Di Modugno, John Saunders, Deborah H. Slee, John P. Williams, Sam R. J. Hoare, Manisha Moorjani
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(24)
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF1 antagonists
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62fe3390acd888ced83d813e4ac50c4a
https://pubmed.ncbi.nlm.nih.gov/21074436
https://pubmed.ncbi.nlm.nih.gov/21074436
Autor:
Raymond S. Gross, John P. Williams, Tanya Joswig, Emily Lin, Stacy Markison, Deborah H. Slee, Marion Lanier, William Kargo, Jaime Piercey, Jose-Luis Diaz, Zhiyong Luo, John E. Tellew, Zhihong O’Brien, Marilyn Zhao, Siobhan Malany, Kayvon Jalali, Mark Santos, Sandra M. Lechner, Ajay Madan, Xiaohu Zhang, Jenny Wen, Yongsheng Chen, Manisha Moorjani, Robert E. Petroski, María I. Crespo, John Saunders
Publikováno v:
Journal of medicinal chemistry. 52(3)
In the present article, we report on a strategy to improve the physical properties of a series of small molecule human adenosine 2A (hA2A) antagonists. One of the aromatic rings typical of this series of antagonists is replaced with a series of aliph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aae503fc7029e4651564ca3936c005ae
https://pubmed.ncbi.nlm.nih.gov/19140664
https://pubmed.ncbi.nlm.nih.gov/19140664
Autor:
Stacy Markison, Sandra M. Lechner, John Saunders, John P. Williams, Silvia Gual, Siobhan Malany, Jaimie K. Rueter, Maria Prat, Raymond S. Gross, Julio C. Castro-Palomino, Tanya Joswig, Kayvon Jalali, Zhiyang Zuo, Manisha Moorjani, Deborah H. Slee, Jose-Luis Diaz, Robert E. Petroski, María I. Crespo, Chun Yang, Yang Sai, Emily Lin, Zhihong O’Brien, Marion Lanier, Xiaohu Zhang, Jenny Wen, Mark Santos, Yongsheng Chen
Publikováno v:
Journal of medicinal chemistry. 51(6)
Previously we have described a series of novel A 2A receptor antagonists with excellent water solubility. As described in the accompanying paper, the antagonists were first optimized to remove an unsubstituted furyl moiety, with the aim of avoiding t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::226a608572d86ea3081c27e5732dbbd6
https://pubmed.ncbi.nlm.nih.gov/18307293
https://pubmed.ncbi.nlm.nih.gov/18307293
Autor:
Silvia Gual, Chun Yang, Yang Sai, Kayvon Jalali, Sandra M. Lechner, Marion Lanier, Mark Santos, Yongsheng Chen, Maria Prat, Julio C. Castro-Palomino, John Saunders, Stacy Markison, John P. Williams, Emily Lin, Jaimie K. Rueter, Jose-Luis Diaz, María I. Crespo, Zhiyang Zuo, Manisha Moorjani, Deborah H. Slee, Raymond S. Gross, Xiaohu Zhang, Siobhan Malany
Publikováno v:
Journal of medicinal chemistry. 51(6)
Previously we have described a novel series of potent and selective A2A receptor antagonists (e.g., 1) with excellent aqueous solubility.(1) While these compounds are efficacious A2A antagonists in vivo, the presence of an unsubstituted furyl moiety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::635873e0540ea30701b581ce36af9624
https://pubmed.ncbi.nlm.nih.gov/18307292
https://pubmed.ncbi.nlm.nih.gov/18307292
Autor:
Zhihong O’Brien, Marion Lanier, Silvia Gual, Siobhan Malany, Manisha Moorjani, John Saunders, Julio C. Castro-Palomino, María I. Crespo, Maria Prat, Sandra M. Lechner, John P. Williams, Deborah H. Slee, Jenny Wen, Xiaohu Zhang, Yongsheng Chen, Stacy Markison, Jose-Luis Diaz, Jaimie K. Rueter, Mark Santos, Emily Lin, Raymond S. Gross, Tanya Joswig
Publikováno v:
Journal of medicinal chemistry. 51(3)
Potent adenosine hA2A receptor antagonists are often accompanied by poor aqueous solubility, which presents issues for drug development. Herein we describe the early exploration of the structure-activity relationships of a lead pyrimidin-4-yl acetami
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df191dacdb02a718b9d6e636b427da95
https://pubmed.ncbi.nlm.nih.gov/18189346
https://pubmed.ncbi.nlm.nih.gov/18189346