Výsledky vyhledávání - "Sandra J. Lobbestael"

Safety of Tacrine: Clinical Trials, Treatment IND, and Postmarketing Experience

Autor: Dale Kraemer, Margaret J. Knapp, James P. Symons, Richard DeJong, William G. Berghoff, Mark W Pierce, Sandra J. Lobbestael, Faye A. Luscombe, Stephen I. Gracon, Stuart L. Dombey

Publikováno v: Alzheimer Disease & Associated Disorders. 12:93-101

The safety of tacrine (Cognex), a centrally active, reversible acetylcholinesterase inhibitor approved in 1993 for the treatment of mild to moderate dementia of the Alzheimer type, was evaluated in 2,706 patients with Alzheimer disease (AD) in clinic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2bbc1ec9cc9422b9f38612b98913b2b
https://doi.org/10.1097/00002093-199806000-00007

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N-Phenyl-N'-pyridinylureas as anticonvulsant agents

Autor: Michael R. Pavia, Fred M. Hershenson, Charles Taylor, David L. Miskell, Sandra J. Lobbestael

Publikováno v: Journal of Medicinal Chemistry. 33:854-861

A series of N-phenyl-N'-pyridinylureas was examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N'-(4-pyridinyl)urea series, with 37 exhibiting the best overal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03bd3341823e62ea9fcd037c06ea0bff
https://doi.org/10.1021/jm00164a061

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Synthesis and metabolic profile of Cl-966: A potent, orally-active inhibitor of GABA uptake

Autor: Louis L. Radulovic, Ann E. Black, Tsun Chang, Susan M. Bjorge, Michael R. Pavia, Thomas F. Woolf, Sandra J. Lobbestael, David Nugiel, Vlad E. Gregor, Howard N. Bockbrader

Publikováno v: Drug Development Research. 21:189-193

A lipophilic derivative of the known GABA uptake inhibitor guvacine has been prepared. The synthesis of this compound, [1-]2-bis 4-(trifluoromethyl)]phenyl[-methoxy]ethyl[- 1,2,5,6-tet-rahydro-3-pyridine carboxylic acid, monohydrochloride, Cl-966, is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f972185a623e64f69aa5672d4a69f242
https://doi.org/10.1002/ddr.430210305

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Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake

Autor: Charles Taylor, Roy D. Schwarz, Daniel Ray Mayhugh, Vlad E. Gregor, Laura J. Brahce, Sandra J. Lobbestael, Mark G. Vartanian, Michael R. Pavia, David A. Nugiel

Publikováno v: Journal of medicinal chemistry. 35(22)

The introduction of lipophilic groups onto the ring nitrogen of nipecotic acid and guvacine, two known GABA uptake inhibitors, afforded potent, orally-active anticonvulsant drugs. A series of compounds is reported which explores the structure-activit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25779b13c5848f801788940f240f3cbf
https://pubmed.ncbi.nlm.nih.gov/1433224

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6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents

Autor: Sandra J. Lobbestael, Michael R. Pavia, Charles Taylor

Publikováno v: Journal of Medicinal Chemistry. 32:1237-1242

The anticonvulsant effect of a series of 6-alkoxy-N,N-disubstituted-2-pyridinamines is described. An investigation was carried out to optimize the activity/side-effect ratio in this series of compounds. The most desirable profile was seen with 1-[6-(

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa48bcfaa7a952cc7b396107e4d82a6d
https://doi.org/10.1021/jm00126a015

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