Výsledky vyhledávání - "Anthony Jerome Thomas"

Identification and Characterization of m1 Selective Muscarinic Receptor Antagonists

Autor: D.W. Moreland, Juan C. Jaen, Penvose-Yi, Roy D. Schwarz, C.E. Augelli-Szafran, C. J. Blankley, Anthony Jerome Thomas, C.B. Nelson

Publikováno v: Journal of Medicinal Chemistry. 42:356-363

A series of esters of 1,4-disubstituted tetrahydropyridine carboxylic acids (I) has been synthesized and characterized as potential m1 selective muscarinic receptor antagonists. The affinity of these compounds for the five human muscarinic receptor s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::99ae9fbcb3fa6b3d09c07d2e2341d960
https://doi.org/10.1021/jm980067l

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(±)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oximes: Potent muscarinic agonists

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

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Z-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes as potential m1-subtype selective muscarinic agonists

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

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Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists

Autor: Haile Tecle, Roy D. Schwarz, D.W. Moreland, Anthony Jerome Thomas, T. Mirzadegan, Carolyn J. Spencer, Juan C. Jaen

Publikováno v: Life Sciences. 56:923-929

Aspartate 103 (D103) in the third transmembrane domain of the Hm2 receptor was mutated to glutamate (D103E), asparagine (D103N), or alanine (D103A). As measured by [3H]-NMS, no significant binding was observed in D103A, while a 2-fold decrease in lig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0da912d0653d09e181b6524aaf085a2e
https://doi.org/10.1016/0024-3205(95)00029-6

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Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5

Autor: Susan Fisher, Anthony Jerome Thomas, Sharie L. Myers, Michael R. Pavia, Walter H. Moos, Kathryn B. Sanders, Robert E. Davis, Linda L. Coughenour

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 2:803-808

There is considerable interest in muscarinic acetylcholine receptor (mAChR) subtype selective agents as cholinomimetics for the treatment of senile dementia of the Alzheimer's type (SDAT). A series of substituted analogs similar to the muscarinic ago

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0756b300258b502df83d79675763c24d
https://doi.org/10.1016/s0960-894x(00)80535-1

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Acetylcholine releasing agents as cognition activators. Chemistry and pharmacology of a series of ureas

Autor: Walter H. Moos, Roy D. Schwarz, Fred M. Hershenson, James P. Symons, Anthony Jerome Thomas, John G. Marriott, Carolyn J. Spencer, Jeffrey Alan Kester, Donald E. Butler, Robert E. Davis

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 2:855-860

We have sought to improve upon the activity of the well known AcCh-releasing agents, 4-aminopyridine and 3,4-diaminopyridine. This work has led to the discovery of a series of ureas with AcCh-releasing properties. From this series, compound 5 has eme

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::966b1c82944375c39ee9e2be708d1d46
https://doi.org/10.1016/s0960-894x(00)80544-2

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CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis, and preclinical pharmacology

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

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