Výsledky vyhledávání - "Leander Merritt"

1,2,5-Thiadiazole Analogues of Aceclidine as Potent m1 Muscarinic Agonists

Autor: David Brunsting, Celia Ann Whitesitt, Michael D. B. Swedberg, John S. Ward, David O. Calligaro, Per Sauerberg, Charles H. Mitch, Preben H. Olesen, Lone Jeppesen, Harlan E. Shannon, Malcolm J. Sheardown, Leander Merritt, Franklin Porter Bymaster

Publikováno v: Journal of Medicinal Chemistry. 41:379-392

The acetyl group of the muscarinic agonist aceclidine 4 was replaced by various 1,2,5-thiadiazoles to provide a new series of potent m1 muscarinic agonists 17 and 18. Optimal m1 muscarinic agonist potency was achieved when the 1,2,5-thiadiazole subst

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4cc0f41d1cb7d6df1b72a892a07e3dd
https://doi.org/10.1021/jm970125n

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Isoarecolones and arecolones: selective central nicotinic agonists that cross the blood-brain barrier

Autor: John S. Ward, Leander Merritt, David O. Calligaro, Frank P. Bymaster

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:573-578

Isoarecolones and arecolones bearing different ketone substituents were synthesized and their affinities at central muscarinic and nicotinic receptors determined. The compounds were selective for nicotinic receptors, produced appropriate nicotinic re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::46d3c896449688a560189472b63d57d4
https://doi.org/10.1016/s0960-894x(01)80157-8

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Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore

Autor: Tage Honore, V. J. Klimkowski, B.D. Sawyer, Michelle Lamb, Harlan E. Shannon, Preben H. Olesen, Charles H. Mitch, Leander Merritt, Franklin Porter Bymaster, John S. Ward

Publikováno v: Journal of Medicinal Chemistry. 35:4011-4019

A series of 3-(3-substituted-pyrazinyl)-1,2,5,6-tetrahydro-1-methylpyridines were synthesized and found to have high affinity for central muscarinic receptors. The ability of some of these compounds to inhibit the electrically stimulated twitch of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7678eac8eaefbd43093f1a08fce3fb7
https://doi.org/10.1021/jm00100a005

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The convergent syntheses of pyrazinyl and quinoxalinyl phenylmethanones from 2-lithio pyrazines and quinoxalines

Autor: Leander Merritt, John S. Ward

Publikováno v: Journal of Heterocyclic Chemistry. 28:765-768

Pyrazines and quinoxalines bearing 2-substituents that direct ortho metalation reacted with lithium 2,2,6,6-tetramethylpiperidide to produce 2-substituted-3-lithiopyrazines and quinoxalines. These lithio reagents reacted with N-methoxy-N-methylbenzam

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e209c08917d3237815b885cf128c3cf0
https://doi.org/10.1002/jhet.5570280336

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The improved convergent syntheses of arecolones and isoarecolone

Autor: Leander Merritt, John S. Ward

Publikováno v: Journal of Heterocyclic Chemistry. 27:1709-1712

Good yields of arecolone and isoarecolone were obtained by treating the N,O-dimethylamides of arecaidine and isoarecaidine, respectively, with methylmagnesium chloride. Other substituted arecolones were synthesized by this same strategy.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1105ccfff17326038de714395a47152e
https://doi.org/10.1002/jhet.5570270636

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Inverse isostere strategies in the development of cholinergic agonists with multiple therapeutic potentials

Autor: Charles H. Mitch, John S. Ward, Michael D. B. Swedberg, Preben H. Olesen, Harlan E. Shannon, Malcolm J. Sheardown, Franklin Porter Bymaster, Leander Merritt, Per Sauerberg, David O. Calligaro

Publisher Summary This chapter discusses inverse isostere strategies in the development of cholinergic agonists with multiple therapeutic potentials. Based on cholinergic hypothesis of dementia, strategies for the enhancement of cholinergic transmiss

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9e29cd6fc78e0afc82289764eae6cc0a
https://doi.org/10.1016/s0165-7208(97)80089-x

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Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles

Autor: Jack B. Deeter, David O. Calligaro, Per Sauerberg, Harlan E. Shannon, Leander Merritt, Franklin Porter Bymaster, Steven C. Peters, John S. Ward, Swedberg, B.D. Sawyer, Malcolm J. Sheardown, Charles H. Mitch, Preben H. Olesen

Publikováno v: Journal of medicinal chemistry. 38(18)

In an attempt to improve upon the M1 agonist activity of the selective M1 agonist xanomeline and related compounds, the M1 muscarinic efficacies and potencies of 3- and 6-substituted pyrazinylazacycles were varied by changing both the 3- and 6-substi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b8629d2e635a44b7a60368265d2ae57
https://pubmed.ncbi.nlm.nih.gov/7658434

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Steric and electronic requirements for muscarinic receptor-stimulated phosphoinositide turnover in the CNS in a series of arecoline bioisosteres

Autor: Scott Roknich, Steven James Quimby, William S. Messer, Per Sauerberg, Dan O. Ngur, John S. Ward, Leander Merritt, Wayne Hoss, Charles H. Mitch

Publikováno v: Biochemical and biophysical research communications. 187(3)

A series of arecoline derivatives was utilized to assess steric and electronic effects important for activating muscarinic receptors in the CNS. Arecoline derivatives in which the methyl ester moiety was replaced by hexyloxy-1,2,5-oxadiazole (2b), he

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70ef1e05ccf8ae3288e360c8503ae871
https://pubmed.ncbi.nlm.nih.gov/1329735

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