31951-25-4Relevant academic research and scientific papers
Synthetic studies to the octahydrobenzo[f]quinoline system
Tagmatarchis, Nikos,Katerinopoulos, Haralambos E.
, p. 983 - 985 (1996)
An improved procedure to 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines is reported giving single intermediate products and higher total yields.
2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS
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Page/Page column 194-195, (2008/06/13)
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
N-(iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: Synthesis and adrenergic and dopaminergic activity studies
Tagmatarchis, Nikos,Thermos, Kyriaki,Katerinopoulos, Haralambos E.
, p. 4165 - 4170 (2007/10/03)
A series of N-(iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines was synthesized and assayed in vitro for their dopaminergic and α-adrenergic activity. Structure-activity relationship (SAR) analysis revealed that the tested benzoquinolines exhibited activity at the D1 rather than the D2 receptor sites in contrast to the D2 receptor subfamily activity reported for their aminotetralin congeners. N-Iodopropenyl substitution was apparently a decisive factor for D1 activity independent of ring substitution pattern. Considering the structural factors influencing α-adrenergic activity, in a general trend, N-iodopropenyl analogues were α1-active, with the ring- hydroxylated congeners exhibiting the highest affinity. Affinity to the α2 receptor was even higher with no detectable trend of SAR. However, a combination of the linear arrangement of the [g]-ring system, combined with the ring hydroxyl and the N-iodopropenyl substitution in compound 5c, resulted in a significant enhancement of α2 activity in this series as demonstrated by an IC50 value of 0.5 nM. A new synthetic approach to the [g]benzoquinoline system is also described.
Hexahydrobenzo (f) quinolinones as 5-alpha-reductase inhibitors
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, (2008/06/13)
The invention relates to 1,2,3,4,5,6-hexahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds, and their use as steroid 5α-reductase inhibitors.
HEXAHYDROBENZO[F]QUINOLINONES
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, (2008/06/13)
The invention relates to 1,2,3,4,5,6-hexahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds, and their use as steroid 5alpha-reductase inhibitors.
