Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Jason Speake"'
Autor:
Stéphanie Braillard, Jason Speake, Sandra Carvalho, Yvonne Freund, Gavin A. Whitlock, Guy Caljon, Bakela Nare, Paul Alan Glossop, Victoriano Corpas-López, Fabio Zuccotto, Louis Maes, Davide Bello, Ian H. Gilbert, Susan Wyllie, Bharathi Pandi, Iva Lukac, Robert T. Jacobs, Magali Van den Kerkhof, Vanessa Yardley, Charles E. Mowbray, Richard J. Wall, Stephen Patterson
Publikováno v:
Journal of Medicinal Chemistry
Journal of medicinal chemistry
Journal of medicinal chemistry
Visceral leishmaniasis (VL) is a parasitic disease endemic across multiple regions of the world and is fatal if untreated. Current therapies are unsuitable, and there is an urgent need for safe, short-course, and low-cost oral treatments to combat th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f1617c4ad5bb29f16cf3dd4c592af7f
https://doi.org/10.1021/acs.jmedchem.1c01437
https://doi.org/10.1021/acs.jmedchem.1c01437
Autor:
John E. Jett, Merouane Bencherif, Rao Akireddy, Jon-Paul Strachan, Jason Speake, Bhatti Balwinder Singh, Lan Miao, Murthy Srinivasa, Mazurov Anatoly A, David C. Kombo, Ronald Heemstra
Publikováno v:
European Journal of Medicinal Chemistry. 86:60-74
We have synthesized a novel series of compounds, 3,6-diazabicyclo[3.1.1]heptane-3-carboxamides, targeting both the α4β2 and α6/α3β2β3 nAChRs. Members of the obtained chemical library are partial or full agonists at both the high sensitivity (α
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0647db59559737fc236a42acf8323a1f
https://doi.org/10.1016/j.ejmech.2014.08.019
https://doi.org/10.1016/j.ejmech.2014.08.019
Autor:
Steve Toler, Rachit N. Jain, Kartik Tallapragada, Joseph Chewning, Jason Speake, Mazurov Anatoly A, David C. Kombo, Terry Hauser
Publikováno v:
Journal of Chemical Information and Modeling. 53:327-342
The pharmacokinetic and safety profiles of clinical drug candidates are greatly influenced by their requisite physicochemical properties. In particular, it has been shown that 2D molecular descriptors such as fraction of Sp3 carbon atoms (Fsp3) and n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fa09c5375b974b8d09e4c1bf66ab52e
https://doi.org/10.1021/ci300445e
https://doi.org/10.1021/ci300445e
Autor:
Terry Hauser, Kristen G. Jordan, Yun-De Xiao, Patrick M. Lippiello, Merouane Bencherif, John W. James, Jason Speake, Sharon R. Letchworth, Jiahui Zhang, Mazurov Anatoly A, Phil S. Hammond, Katherine M. Van Dyke
Publikováno v:
European Journal of Pharmaceutical Sciences. 47:813-823
Nicotinic α4β2* agonists are known to be effective in a variety of preclinical pain models, but the underlying mechanisms of analgesic action are not well-understood. In the present study, we characterized activation and desensitization properties
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4da1939aeae4a385b816d5df778c4c6a
https://doi.org/10.1016/j.ejps.2012.09.014
https://doi.org/10.1016/j.ejps.2012.09.014
Autor:
Jason Speake, Lan Miao, Jenny Z. Zhang, Gatto Gregory J, Philip S. Hammond, Srinivasa Rao Akireddy, Daniel Yohannes, Mazurov Anatoly A, Murthy Srinivasa, David C. Kombo, Kristen G. Jordan, Bhatti Balwinder Singh, Jon-Paul Strachan, Terry Hauser, Miller Craig H, Yun-De Xiao
Publikováno v:
Journal of Medicinal Chemistry. 55:9181-9194
Diversification of essential nicotinic cholinergic pharmacophoric elements, i.e., cationic center and hydrogen bond acceptor, resulted in the discovery of novel potent α4β2 nAChR selective agonists comprising a series of N-acyldiazabicycles. Core c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40bba2286b1c5633da9a288aa65744a9
https://doi.org/10.1021/jm3006542
https://doi.org/10.1021/jm3006542
Autor:
William Scott Caldwell, Terry Hauser, Daniel Yohannes, Kartik Tallapragada, Mazurov Anatoly A, Philip S. Hammond, David C. Kombo, Jason Speake, Joseph Chewning
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1179-1186
Based on pharmacophore elucidation and docking studies on interactions of benzylidene anabaseine analogs with AChBPs and α7 nAChR, novel spirodiazepine and spiroimidazoline quinuclidine series have been designed. Binding studies revealed that some o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::983c815a1d7a3c386ee1ec6cbf1df81f
https://doi.org/10.1016/j.bmcl.2011.11.090
https://doi.org/10.1016/j.bmcl.2011.11.090
Publikováno v:
Journal of medicinal chemistry. 54(23)
Efforts in the design and discovery of selective α7 nicotinic acetylcholine receptor (nAChR) agonists were both facilitated and hampered by observation that ligands can show dual affinity at both the 5-HT3 receptor (5-HT3R) and nAChR. 1 The 5-HT3R a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1277c58955e2246e5d4a7a01c5e3a5bd
https://pubmed.ncbi.nlm.nih.gov/21919481
https://pubmed.ncbi.nlm.nih.gov/21919481
Autor:
Yuping Gong, Donavon McConn, Beth Beaudet, Melanie Tallman, Jason Speake, Diane Ignar, Jeffrey Krise
Publikováno v:
Pharmaceutical Research; Jun2007, Vol. 24 Issue 6, p1138-1144, 7p