143121-58-8Relevant articles and documents
Conformer interconversion in the excited state of constrained tryptophan derivatives
McMahon, Lloyd P.,Yu, Hong-Tao,Vela, Marco A.,Morales, Guillermo A.,Shui, Li,Fronczek, Frank R.,McLaughlin, Mark L.,Berkley, Mary D.
, p. 3269 - 3280 (1997)
The conformer model of tryptophan photophysics ascribes the multiple fluorescence lifetimes to ground-state heterogeneity. It is usually assumed that the different conformers do not interconvert in the excited state. Previous studies of two constrained tryptophan derivatives supported this assumption (Colucci, W. J.; Tilstra, L.; Sattler, M. C.; Fronczek, F. R.; Barkley, M. D. J. Am. Chem. Soc. 1990, 112, 9182-9190; Yu, H.-T.; Vela, M. A.; Fronczek, F. R.; McLaughlin, M. L.; Barkley, M. D. J. Am. Chem. Soc. 1995, 117, 348-357). Five constrained derivatives have been synthesized and shown to undergo conformer inversion during the lifetime of the excited state. All derivatives have two ground-state conformations as determined by X-ray crystallography, molecular mechanics calculations, and 1H-NMR. Fluorescence lifetime data were fit to single-and double-exponential models and to a reversible two-state excited-state reaction model. 2-Ammo-1,2-dihydrocyclopenta[b]indole-2-carboxylic acid has a single-exponential decay consistent with conformer inversion much faster than fluorescence decay. 1,2,3,4-Tetrahydrocarbazole-3-carboxylic acid, ethyl 1,2,3,4-tetrahydrocarbazole-3-carboxylate, and their 9-methyl derivatives have double-exponential decays with a minor second component of small positive or negative amplitude. Conformer inversion rates of ～107 s-1 were determined by analyzing the fluorescence decay data using the excited-state reaction model. Temperature dependence of the fluorescence lifetimes was measured in H2O and D2O, and solvent quenching rates were calculated from the Arrhenius parameters. The carboxylate and carbonyl functional groups appear to have little effect on solvent quenching of indole fluorescence. Model calculations examining the effect of conformer inversion rate on the decay parameters of a biexponential model indicate that the presence of a small amplitude, short lifetime component may be a good predictor of excited-state conformer interconversion of tryptophans in peptides and proteins.
3-substituted 1,2,3,4-tetrahydrocarbazoles.
Rice,Scott
, p. 308 - 311 (1970)
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METHODS AND MATERIALS FOR INCREASING OR MAINTAINING NICOTINAMIDE MONONUCLEOTIDE ADENYLYL TRANSFERASE-2 (NMNAT2) POLYPEPTIDE LEVELS
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, (2020/09/08)
This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
2,3,4,9-TETRAHYDRO-1H-CARBAZOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Page/Page column 44, (2008/06/13)
The invention relates to novel tetrahydro-lH-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
