108061-47-8Relevant articles and documents
Binding of β-carbolines at 5-HT2 serotonin receptors
Grella, Brian,Teitler, Milt,Smith, Carol,Herrick-Davis, Katharine,Glennon
, p. 4421 - 4425 (2003)
A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-β-carbolines was examined at 5-HT2A and 5-HT2C serotonin receptors. Whereas most of the methoxy-substituted derivatives typically displayed affinities similar to their unsubstituted parents, certain (particularly 8-substituted) bromo derivatives displayed enhanced affinity. A binding profile was obtained for selected β-carbolines.
TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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, (2021/02/12)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.
Tetrahydrocarboline analogs as MCH-1 antagonists
Henderson, Alan J.,Deering, Dustin,Grabowski, James F.,Hadden, Mark,Jiang, Xiaowu,Khmelnitsky, Yuri,Luche, Michele,Surman, Matthew D.,Cheetham, Sharon,Vickers, Steven,Viggers, Jean,Guzzo, Peter R.
scheme or table, p. 7024 - 7028 (2011/01/05)
A new series of tetrahydrocarbolines with potent MCH-1 antagonist activity were synthesized, using a conformationally constrained design approach towards optimizing pharmacokinetic properties. Two compounds from this series were progressed to a 5-day diet-induced obesity mouse screening model to evaluate their potential as weight loss agents. Both compounds produced a highly significant reduction in weight, which was attributed to their improved pharmacokinetic profile.
Synthesis of didemnolines A-D, N9-substituted β-carboline alkaloids from the marine ascidian Didemnum sp.
Schumacher, Robert W.,Davidson, Bradley S.
, p. 935 - 942 (2007/10/03)
Didemnolines A-D (1-4) were synthesized and their structures were confirmed through comparisons of data for the synthetic material with those obtained for natural 1-4. The synthesis of didemnolines A (1) and C (3) involved the coupling of 1-[(benzyloxy)methyl]-4-chloromethyl-5- (thiomethyl)imidazole (6) with 7-bromo-β-carboline (5), while didemnolines B (2) and D (4) were formed through the analogous coupling of 6 with norharmon (7). Intermediate 6 was efficiently prepared from 1-[(benzyloxy)methyl]- 2,4,5-tribromoimidazole using a sequential one-pot halogen-metal exchange reaction and 7-Br-β-carboline was synthesized using a new approach.