Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Lauffer David Jeffrey"'
Autor:
R.D. Schwan, Anthony Jerome Thomas, D.W. Moreland, Haile Tecle, Juan C. Jaen, T. Mirzadegan, Lauffer David Jeffrey, Charlotte Raby, David Eubanks, Mark R. Brann, Robert E. Davis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:637-642
Synthesis and SAR of a new class of 1-azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oxime muscarinic agonists are described. Depending on the geometry of the C=N and C=C bonds, subnanomolar potency and/or high efficacy are achiev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d19db98ce421d0af342857b2b965ea7f
https://doi.org/10.1016/0960-894x(95)00087-a
https://doi.org/10.1016/0960-894x(95)00087-a
Autor:
Haile Tecle, Robert E. Davis, Roy D. Schwarz, Bradley William Caprathe, T. Mirzadegan, Stephen Douglas Barrett, Walter H. Moos, Lauffer David Jeffrey, Juan C. Jaen, Anthony Jerome Thomas, D.W. Moreland, Michael R. Pavia, C.E. Augelli-Szafran
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:631-636
The synthesis and SAR of a series of Z-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes are described. The biochemistry and pharmacology of PD 142505 (5b), an oxime with pronounced functional ml selectivity, are highlighted.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8357932845da7b87b82fc5231351818d
https://doi.org/10.1016/0960-894x(95)00086-9
https://doi.org/10.1016/0960-894x(95)00086-9
Autor:
Michael R. Pavia, Haile Tecle, Lauffer David Jeffrey, Walter H. Moos, D.W. Moreland, Roy D. Schwarz, Robert E. Davis, T. Mirzadegan
Publikováno v:
Life Sciences. 52:505-511
The synthesis of a series of potent and efficacious 1-azabicyclo[2.2.1]heptan-3-one oxime muscarinic agonists is described. The oximes have extended appendages designed to span the cavity defined by the seven transmembrane helices of the muscarinic r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ea317027bf919023b13e01ff72aeb09
https://doi.org/10.1016/0024-3205(93)90308-p
https://doi.org/10.1016/0024-3205(93)90308-p
Autor:
Robert E. Davis, Haile Tecle, Bradley William Caprathe, Mark R. Emmerling, Anthony Jerome Thomas, Michael J. Callahan, Roy D. Schwarz, C.B. Nelson, Juan C. Jaen, Katharyn Spiegel, P.D. Doyle, Stephen Douglas Barrett, Charlotte Raby, D.W. Moreland, W Lipiniski, Carolyn J. Spencer, T. Mirzadegan, Lauffer David Jeffrey
Publikováno v:
Pharmaceutica acta Helvetiae. 74(2-3)
The five muscarinic receptor subtypes (M 1 –M 5 ) are characterized by seven helices that define a transmembrane cavity which serves as the binding pocket for agonists and antagonists. The five cavities appear to be topographically different enough
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f7425e6c1f719eff79baa6e2de826cd
https://pubmed.ncbi.nlm.nih.gov/10812951
https://pubmed.ncbi.nlm.nih.gov/10812951
Autor:
C.E. Augelli-Szafran, Mark R. Brann, Charlotte Raby, Juan C. Jaen, Haile Tecle, T. Mirzadegan, Patricia D. Doyle, D.W. Moreland, David Eubanks, Roy D. Schwarz, Robert E. Davis, Walter H. Moos, Bradley William Caprathe, C.B. Nelson, and Anthony J. Thomas, Michael J. Callahan, William Lipiniski, Carolyn J. Spencer, Lauffer David Jeffrey, Stephen Douglas Barrett, Michael R. Pavia
Publikováno v:
Journal of medicinal chemistry. 41(14)
The synthesis and SAR of a series of (Z)-(+/-)-1-azabicyclo[2.2. 1]heptan-3-one, O-(3-aryl-2-propynyl)oximes are described. The biochemistry and pharmacology of 24Z (PD 142505) and its enantiomers are highlighted. 24Z is functionally an m1-selective
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2dcd1a3da4e6e0e17b8b08d4efdff44c
https://pubmed.ncbi.nlm.nih.gov/9651157
https://pubmed.ncbi.nlm.nih.gov/9651157
Autor:
D.W. Moreland, Haile Tecle, C.B. Nelson, Carolyn J. Spencer, Roy D. Schwarz, P. Doyle, Stephen Douglas Barrett, Mark R. Brann, Michael J. Callahan, David Eubanks, Lauffer David Jeffrey, Charlotte Raby, Juan C. Jaen, Robert E. Davis, L. Lauffer, William J. Lipinski
Publikováno v:
Life sciences. 56(11-12)
PD 151832 is a potent partial muscarinic agonist that displays a high level of functional selectivity for the muscarinic m1 receptor subtype, as evidenced by its selective stimulation of PI turnover and cellular metabolic activity in transfected Hm1-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92ba39604a9481ff5700273f9bc67663
https://pubmed.ncbi.nlm.nih.gov/10188784
https://pubmed.ncbi.nlm.nih.gov/10188784
Autor:
David T. Dudley, Charlotte Raby, William J. Lipinski, Roy D. Schwarz, Juan C. Jaen, Michael J. Callahan, Phillip A. Reece, Haile Tecle, Robert Davis, Lauffer David Jeffrey
Publisher Summary Senile dementia of Alzheimer type (AD) is a progressive neurodegenerative disease of unknown etiology. AD and related dementias are characterized by significant neuronal pathology in discrete cortical and subcortical brain regions.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a816c4b3749dc1f796017e4944644c89
https://doi.org/10.1016/s0079-6123(08)62430-9
https://doi.org/10.1016/s0079-6123(08)62430-9
Autor:
Haile Tecle, T. Mirzadegan, Juan C. Jaen, D.W. Moreland, Roy D. Schwarz, Robert E. Davis, Lauffer David Jeffrey, Charlotte Raby, Anthony Jerome Thomas
Publikováno v:
Life Sciences. 56:1003
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::69b5d1f8b0d1b30d6c7bcd0ccbac8bf8
https://doi.org/10.1016/0024-3205(95)93719-u
https://doi.org/10.1016/0024-3205(95)93719-u
Publikováno v:
Life Sciences. 52:561
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bd4fc889622a2a52fcfde175fc176d17
https://doi.org/10.1016/0024-3205(93)90339-5
https://doi.org/10.1016/0024-3205(93)90339-5