Zobrazeno 1 - 10 of 28 pro vyhledávání: '"Margaret M. Schweri"'
1
Synthesis and Pharmacology of Site-Specific Cocaine Abuse Treatment Agents: Restricted Rotation Analogues of Methylphenidate
Autor: Xiaocong Ye, Howard M. Deutsch, Margaret M. Schweri, Deog-Il Kim
Publikováno v: Journal of Medicinal Chemistry. 50:2718-2731
A series of threo-1-aza-3 or 4-substituted-5-phenyl[4.4.0]decanes (quinolizidines), which were envisioned as restricted rotational analogues (RRAs) of methylphenidate (MP), was synthesized and tested for inhibitory potency against [(3)H]WIN35,428, [3
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69c81603111429fb1d99cd89bc9fdc91
https://doi.org/10.1021/jm061354p
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2
Biochemical and Behavioral Characterization of Novel Methylphenidate Analogs
Autor: H M Deutsch, A T Massey, S G Holtzman, Margaret M. Schweri
Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 301:527-535
As part of a project to develop treatment agents for cocaine abuse, (+/-)-threo-methylphenidate (TMP) and 11 analogs were characterized biochemically and behaviorally to assess their potential as anti-cocaine medications. The compounds contained aryl
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a77be3e75d9072073f2787e0126221bc
https://doi.org/10.1124/jpet.301.2.527
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3
Synthesis and pharmacology of site specific cocaine abuse treatment agents: a new synthetic methodology for methylphenidate analogs based on the Blaise reaction
Autor: Xiaocong Ye, Qing Shi, Margaret M. Schweri, Howard M. Deutsch, Zhanzhu Liu
Publikováno v: European Journal of Medicinal Chemistry. 36:303-311
In order to make new analogs of the dopamine (DA) uptake inhibitor methylphenidate, a synthetic methodology based on the Blaise reaction was developed. The reaction between alpha-bromophenylacetic acid esters, zinc and alpha-cyano-omega-mesylates gav
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e62fe8db6f1177ff3d7bceb207c7e61
https://doi.org/10.1016/s0223-5234(01)01230-2
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4
Synthesis and Pharmacology of Site-Specific Cocaine Abuse Treatment Agents: 2-(Aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane Dopamine Uptake Inhibitors
Autor: Margaret M. Schweri, Kikue S. Burnham, Liang Zhang, Stephan G. Holtzman, Abhay K. Deshpande, David M. Collard, Howard M. Deutsch
Publikováno v: Journal of Medicinal Chemistry. 42:882-895
As part of a program to develop site-specific medications for cocaine abuse, a series of 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane derivatives was synthesized and tested for inhibitory potency in [3H]WIN 35,428 binding and [3H]dopami
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::790585d6dbc7ef9114645c9608693183
https://doi.org/10.1021/jm980566m
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5
Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on Threo-methylphenidate and its analogs
Autor: Howard M. Deutsh, Margaret M. Schweri, Quing Shi, Mark Froimowitz, Robert Glaser, Clifford George, Itay Adin, Kuo-Ming Wu
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:1213-1218
N-methyl derivatives of methylphenidate and four analogs were synthesized and assayed for affinity at the dopamine transporter. The binding affinities of the N-methyl compounds were consistently lower by a factor ranging from 4 to 30 as compared with
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::162dfad65c9946bc258723d78c452fc3
https://doi.org/10.1016/s0960-894x(97)00193-5
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6
Can stimulant binding and dopamine transport be differentiated? Studies with GBR 12783 derivatives
Autor: Margaret M. Schweri, Howard M. Deutsch
Publikováno v: Life Sciences. 55:PL115-PL120
Both 3- and 4-substituted GBR 12783 derivatives were synthesized in an effort to create site-directed cocaine antagonists. The potencies of these compounds to inhibit stimulant ([3H]WIN 35,428) binding and synaptosomal [3H]dopamine uptake were determ
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a1d49351509fdaa1783890eb7214538
https://doi.org/10.1016/0024-3205(94)90061-2
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8
Quantitative structure-activity relationship studies of threo-methylphenidate analogs
Autor: Qing Shi, Howard M. Deutsch, Milind Misra, Xiaocong Ye, Carol A. Venanzi, Zhanzhu Liu, Margaret M. Schweri, Wei Bu, Ewa Gruszecka-Kowalik
Publikováno v: Bioorganicmedicinal chemistry. 18(20)
Complementary two-dimensional (2D) and three-dimensional (3D) Quantitative Structure–Activity Relationship (QSAR) techniques were used to derive a preliminary model for the dopamine transporter (DAT) binding affinity of 80 racemic threo-methylpheni
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::333782933edd836f716cacdb17bab99a
https://pubmed.ncbi.nlm.nih.gov/20846865
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10
The enantiomeric specificity of the antihypertensive activity of 1-(phenylthio)-2-aminopropane, a synthetic substrate analog for dopamine .beta.-monooxygenase
Autor: Heath H. Herman, James E. Colbert, Lydia C. Fowler, Sheldon W. May, Margaret M. Schweri, Philip A. Husain, Stanley H. Pollock
Publikováno v: Journal of Medicinal Chemistry. 34:1082-1085
We have found that (R,S)-1-(phenylthio)-aminopropane (4a), a synthetic alternate substrate for the terminal enzyme of norepinephrine biosynthesis, dopamine beta-monooxygenase (DBM), is both an indirect sympathomimetic and a potent antihypertensive ag
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90a43321bd564f988244826552d5cec5
https://doi.org/10.1021/jm00107a031
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