Zobrazeno 1 - 10
of 40
pro vyhledávání: '"S W Mascarella"'
Autor:
Anita H. Lewin, S. W. Mascarella, Amanda Gilbert, Herbert H. Seltzman, P. Silinski, Desong Zhong
Publikováno v:
Organicbiomolecular chemistry. 16(31)
The one-carbon carrier of the formate oxidation level derived from the interaction of tetrahydrofolate and formiminoglutamate, which has been tentatively identified as 5-formiminoltetrahydrofolate, has been prepared by chemical synthesis. Treatment o
Autor:
S. W. Mascarella, F. Ivy Carroll, X. Zhang, Judith L. Flippen-Anderson, Philip Abraham, Jeffrey R. Deschamps
Publikováno v:
ARKIVOC, Vol 2010, Iss 4, Pp 96-103 (2010)
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(2S,5S,8R)-Strobamine (+)-1a was synthesized by adding cinnamoyl cyanide 6a to tropinone 3 lithium enolate generated by treatment of (S,S')-alpha, alpha-dimethyldibenzylamide with butyl lithium in the presence of lithium chloride to give (-)-chalcost
Autor:
Juan Pablo Cueva, Frank I. Carroll, Scott P. Runyon, James B. Thomas, Hernán A. Navarro, S. W. Mascarella
Publikováno v:
ACS Medicinal Chemistry Letters. 1:365-369
This report describes the discovery that 1-substituted 4-(3-hydroxyphenyl)piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine and (3R)-3-methyl-4-(3-hydroxy
Autor:
Carroll Fi, Jeffrey R. Deschamps, S. W. Mascarella, Bruce E. Blough, Zhe Nie, Xiaodong Huang, Hernán A. Navarro
Publikováno v:
Journal of Medicinal Chemistry. 49:4589-4594
A series of cyclo-3beta-(4-aminophenyl)-2beta-tropanemethanol analogues (5a-m) possessing varying linker groups between the 2- and 3-position on the tropane ring were synthesized and evaluated for their monoamine transporter binding properties. The r
Autor:
D. M. Zimmerman, S. W. Mascarella, Richard B. Rothman, Carroll Fi, Jim A. Thomas, B. E. Cantrell, Christina M. Dersch, Scott E. Fix
Publikováno v:
Journal of Medicinal Chemistry. 47:1070-1073
In vitro characterization and comparison of JDTic, its dehydroxy analogue and nor-BNI, and its dehydroxy analogue demonstrates that the N-substituted 3,4-dimethyl-(3-hydroxyphenyl)piperidine-derived antagonist, JDTic, relies more heavily on its pheno
Autor:
Jim A. Thomas, Robert N. Atkinson, D. M. Zimmerman, Noelle Vinson, Richard B. Rothman, Christina M. Dersch, Kenneth M. Gigstad, Nivedita Namdev, Scott E. Fix, Jason P. Burgess, Heng Xu, F. I. Carroll, S. W. Mascarella, B. E. Cantrell
Publikováno v:
Journal of Medicinal Chemistry. 45:3524-3530
A library of compounds biased toward opioid receptor antagonist activity was prepared by incorporating N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)morphans as the core scaffold using simultaneous solution phase synthetic methodology. From this lib
Autor:
Razdan Rk, S. W. Mascarella, PJ Crocker, Alison R. Keimowitz, Billy R. Martin, Brian F. Thomas
Publikováno v:
Journal of Medicinal Chemistry. 43:59-70
A novel quantitative structure-activity relationship (QSAR) for the side-chain region of Delta(8)-tetrahydrocannabinol (Delta(8)-THC) analogues is reported. A series of 36 side-chain-substituted Delta(8)-THCs with a wide range of pharmacological pote
Autor:
Carroll Fi, John W. Boja, Michael J. Kuhar, S. W. Mascarella, Anita H. Lewin, Philip Abraham, Pravin Kotian
Publikováno v:
Journal of Medicinal Chemistry. 39:2753-2763
A set of 3 beta-(4'-substituted phenyl)-2 beta-heterocyclic tropanes was designed, synthesized, and characterized. We discovered that these compounds can function as bioisosteric replacements for the corresponding WIN 35,065-2 analogs which possess a
Publikováno v:
Journal of Medicinal Chemistry. 39:471-479
Anandamides are endogenous fatty acid ethanolamides that have been shown to bind to the cannabinoid receptor and possess cannabimimetic activity yet are structurally dissimilar from the classical cannabinoids found in Cannabis sativa. We have employe
Autor:
W. D. Bowen, Wanda Williams, Xu Bai, R. Danso‐Danquah, B. Sine, S. W. Mascarella, X. Zhang, Frank I. Carroll
Publikováno v:
Journal of Medicinal Chemistry. 38:2978-2985
The synthesis and sigma 1 and sigma 2 binding properties of several (+)- and (-)-2-benzyl- and 2-dimethylallyl-2'-substituted-5,9 alpha-dimethyl-6,7-benzomorphans (3 and 4) are presented. In agreement with previously reported binding data for 2-subst