Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Jeffrey S. Albert"'
Autor:
François Godin, Daniel P. Canterbury, Samuel Desjardins, Malken Bayrakdarian, David Austen Perry, Jeffrey S. Albert, Kevin D. Hesp
Publikováno v:
Organic Letters. 20:5336-5339
A practical and asymmetric synthesis of a small-molecule CXCR7 modulator featuring a highly functionalized and hindered tertiary β-amino amide framework is reported. The cornerstone of this strategy relied on the intermediacy of a reactive aziridini
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3aea7c2b43df0533c2d7c956b98592f6
https://doi.org/10.1021/acs.orglett.8b02261
https://doi.org/10.1021/acs.orglett.8b02261
Autor:
Gaochao Tian, William Frietze, Michael W. Wood, Christopher R. Holmquist, Todd Andrew Brugel, William E. Palmer, Hui Xiong, Deidre E. Wilkins, Glen Ernst, William Potts, Lindsay Hinkley, Janet Marie Forst, Xia Wang, Jeffrey S. Albert, Cristobal Alhambra, Gary Steelman, Jeffrey G. Varnes, Gerald Jonak, Don Andisik, Bruce Dembofsky, Chris Allan Veale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1043-1049
A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the natur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc9dfd0d0aa8815e2e21d0c94b006632
https://doi.org/10.1016/j.bmcl.2018.02.029
https://doi.org/10.1016/j.bmcl.2018.02.029
Autor:
Shawn Johnstone, Jeffrey S. Albert
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2239-2258
New strategies to potentially improve drug safety and efficacy emerge with allosteric programs. Biased allosteric modulators can be designed with high subtype selectivity and defined receptor signaling endpoints, however, selecting the most meaningfu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5be7fe59a9635fecff80e97eb8f63339
https://doi.org/10.1016/j.bmcl.2017.03.084
https://doi.org/10.1016/j.bmcl.2017.03.084
Autor:
Gaochao Tian, Xia Wang, Stefan Geschwindner, Clay W Scott, Jeffrey G. Varnes, Janet Marie Forst, Niek Dekker, Jeffrey S. Albert, Christopher R. Holmquist, Michael W. Wood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:197-202
Fragment-based drug design (FBDD) relies on direct elaboration of fragment hits and typically requires high resolution structural information to guide optimization. In fragment-assisted drug discovery (FADD), fragments provide information to guide se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d670568fa102439bf0e61ea059f6dd60
https://doi.org/10.1016/j.bmcl.2015.10.100
https://doi.org/10.1016/j.bmcl.2015.10.100
Autor:
Sjoerd J. Finnema, Jonas Malmquist, Marie Svedberg, Frederic Vallee, Katarina Varnäs, Magnus Schou, Jeffrey S. Albert
Publikováno v:
ACS chemical neuroscience. 9(2)
Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for such measurements on the cholinerg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::909ce4d06e5710ac003282720f7d8894
https://pubmed.ncbi.nlm.nih.gov/29072902
https://pubmed.ncbi.nlm.nih.gov/29072902
Autor:
Henrik Dahllof, Olivier Radresa, Andreas Nolting, Patrick Raboisson, Eva Nyman, Jeffrey S. Albert
Publikováno v:
The Open Pain Journal. 6:137-153
The Transient Receptor Potential A1 (TRPA1) ion channel has evolved in animals to respond to signals from a variety of sensory stimuli. Many structural determinants of its multimodal activation have been identified to date. TRPA1 activities include r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6b34f34f59d5d77bd16a5fa19ff58b7e
https://doi.org/10.2174/1876386301306010137
https://doi.org/10.2174/1876386301306010137
Publikováno v:
Current Topics in Medicinal Chemistry. 13:367-385
During inflammation, several Transient Receptor Potential (TRP) channels are directly or indirectly activated by inflammatory signaling molecules and microenvironmental changes including heat, oxidative conditions or low pH. In either case, specific
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::55591e2e6471b4edb7edc2e38ff8f6b0
https://doi.org/10.2174/1568026611313030012
https://doi.org/10.2174/1568026611313030012
Autor:
Michael W. Wood, Jeffrey S. Albert
Publikováno v:
Targets and Emerging Therapies for Schizophrenia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::601039bcee05621bae44537b211b53c4
https://doi.org/10.1002/9781118309421.ch8
https://doi.org/10.1002/9781118309421.ch8
Autor:
Lindsay Hinkley, James Woods, Hui Xiong, Gerard M. Koether, Reto Gadient, James Kang, John P. McCauley, Thomas R. Simpson, Jeffrey S. Albert, Yan Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1896-1899
The neurokinin-3 (NK3) receptor is regarded as a potential novel target for treating patients with schizophrenia. Herein we report the synthesis and SAR of a series of C3-alkylsulfoxide substituted quinolines as potent NK3 receptor antagonists. These
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc20142e26508893c1123573eadf5f52
https://doi.org/10.1016/j.bmcl.2010.11.003
https://doi.org/10.1016/j.bmcl.2010.11.003