Zobrazeno 1 - 10 of 34 pro vyhledávání: '"Howard M. Deutsch"'
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
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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3
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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4
Solution and Solid-State Conformational and Structural Analysis of the N-Methyl Derivatives of (±)-threo-Methylphenidate, (±)-erythro-Methylphenidate, and (±)-threo-p-Methyl-methylphenidate Hydrochloride Salts
Autor: Kuo-Ming Wu, Robert Glaser, Itay Adin, Dror Shiftan, Howard M. Deutsch, Mark Froimowitz, Clifford George, Qing Shi
Publikováno v: The Journal of Organic Chemistry. 63:1785-1794
The conformational preferences of N-methyl derivatives of the dopamine reuptake blocker threo-methylphenidate [Ritalin] and the p-methyl analogue were determined in the solid state and in solution and that of the erythro isomer in solution. The solid
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5c558d36965bde8706ad8e0eb17d8c6d
https://doi.org/10.1021/jo971063b
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5
[Untitled]
Autor: Don VanDerveer, Kuo-Ming Wu, Qing Shi, Mark Froimowitz, Clifford George, Howard M. Deutsch
Publikováno v: Structural Chemistry. 9:295-303
The crystal structures of the chloride salts of five analogs of threo-methylphenidate have been obtained. Four of these have different substituents on the phenyl ring while the fifth is the ethyl ester of methylphenidate. All five structures have sim
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::11f7485e6e16a54fc5343756f90a0225
https://doi.org/10.1023/a:1022435131188
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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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7
Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling
Autor: Howard M. Deutsch, Christopher K. Surratt, John R. Lever, David J. Lapinsky, Yi Liu, Ranganadh Velagaleti, Yurong Huang, James D. Foster, Nageswari Yarravarapu, Roxanne A. Vaughan, Rejwi Acharya
Publikováno v: Bioorganicmedicinal chemistry. 19(1)
In contrast to tropane-based compounds such as benztropine and cocaine, non-tropane-based photoaffinity ligands for the dopamine transporter (DAT) are relatively unexplored. Towards addressing this knowledge gap, ligands were synthesized in which the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f604d13f4ba81dbb63fbd67ee49ed96
https://pubmed.ncbi.nlm.nih.gov/21129986
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9
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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