Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Said Zamani-Kord"'
Autor:
Paul D. Crowe, Said Zamani-Kord, Bin-Feng Li, Sam R. J. Hoare, Hua Wang, Charles Q. Huang, Siobhan Malany, Wilna J. Moree, Ajay Madan, Fabio C. Tucci, Graham Beaton, Chun Yang, Jianyun Wen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:947-951
Structure–activity relationship studies were conducted to reduce CYP2D6-mediated metabolism in a series of indene H1-antihistamines. Reductions in pKa via incorporation of a β-fluoro substituent or a heteroaryl moiety were shown to reduce contribu
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
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
Autor:
Sam R. J. Hoare, Graham Beaton, Bin-Feng Li, Paul D. Crowe, Said Zamani-Kord, Lisa M. Hernández, Wilna J. Moree, Charles Q. Huang, Jinghua Yu, Hua Wang, Siobhan Malany, Fabio C. Tucci, Chun Yang, Ajay Madan, Aida Sacaan, Robert E. Petroski, Jianyun Wen, Coon Timothy Richard, Margaret J. Bradbury, Kayvon Jalali, Dragan Marinkovic
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(19)
Analogs of the known H(1)-antihistamine R-dimethindene with suitable selectivity for key GPCRs, P450 enzymes and hERG channel were assessed for metabolism profile and in vivo properties. Several analogs were determined to exhibit diverse metabolism.
Autor:
Paul D. Crowe, Chun Yang, Robert E. Petroski, Kayvon Jalali, Coon Timothy Richard, Wilna J. Moree, Sam R. J. Hoare, Bin-Feng Li, Said Zamani-Kord, Hua Wang, Graham Beaton, Siobhan Malany, Jianyun Wen, Ajay Madan, Jinghua Yu
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(8)
A series of indene analogs of the H1-antihistamine (−)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron
Autor:
Fabio C. Tucci, Lisa M. Hernández, Graham Beaton, Ajay Madan, Bin-Feng Li, Margaret J. Bradbury, Robert E. Petroski, Wilna J. Moree, Hua Wang, Dragan Marinkovic, Jinghua Yu, Jianyun Wen, Raymond S. Gross, Siobhan Malany, Florence Jovic, Paul D. Crowe, Said Zamani-Kord, Coon Timothy Richard, Zhihong O’Brien, Aida Sacaan, Sam R. J. Hoare
Publikováno v:
Journal of medicinal chemistry. 52(17)
Analogues of the known H(1)-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzo
Autor:
Graham Beaton, Aixia Sun, Jason Haelewyn, Susan K. Sullivan, Wilna J. Moree, Michael P. Hedrick, Mark Santos, Margaret J. Bradbury, Jenny Wen, Jinghua Yu, Said Zamani-Kord, Coon Timothy Richard, Paul D. Crowe, Lisa M. Hernández, Siobhan Malany, Robert E. Petroski, Bin-Feng Li, Samuel J. Hoare
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
The benzimidazole core of the selective non-brain-penetrating H 1 -antihistamine mizolastine was used to identify a series of brain-penetrating H 1 -antihistamines for the potential treatment of insomnia. Using cassette PK studies, brain-penetrating
Autor:
Wilna J. Moree, Bin-Feng Li, Florence Jovic, Timothy Coon, Jinghua Yu, Raymond S. Gross, Fabio Tucci, Dragan Marinkovic, Said Zamani-Kord, Siobhan Malany, Margaret J. Bradbury, Lisa M. Hernandez, Zhihong O’Brien, Jianyun Wen, Hua Wang, Samuel R. J. Hoare, Robert E. Petroski, Aida Sacaan, Ajay Madan, Paul D. Crowe
Publikováno v:
Journal of Medicinal Chemistry; Sep2009, Vol. 52 Issue 17, p5307-5310, 4p