178174-35-1Relevant academic research and scientific papers
Synthesis of 9-substituted 2,3,4,9-tetrahydro-1H-carbazole derivatives and evaluation of their anti-prion activity in TSE-infected cells
Kimura, Tsutomu,Hosokawa-Muto, Junji,Asami, Kenji,Murai, Toshiaki,Kuwata, Kazuo
supporting information; experimental part, p. 5675 - 5679 (2012/01/02)
2,3,4,9-Tetrahydro-9-[2-hydroxy-3-(1-piperidinyl)propyl] -6-methyl-1H-carbazol-1-one (GJP14) is a novel anti-prion compound that we previously discovered by in silico screening and cellular assay. In this study, a variety of GJP14 derivatives were prepared using pyrrole derivatives, (haloalkyl)oxiranes, and amines, and their anti-prion activity was evaluated in TSE-infected cells. It was found that the tricyclic aromatic ring, a hydroxy group at the 2-position and an amino group at the 3-position of the N-propyl group were the basic requirements for anti-prion activity. The derivatives bearing an N-ortho-halobenzyl group exhibited an improved activity, and the most potent derivative was 8 times as effective as the original lead compound, GJP14.
3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
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, (2008/06/13)
3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3and R4independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.
Synthesis and in vitro antitumor activity evaluation of 9-substituted 1,2,3,4-tetrahydrocarbazoles
Grasso,Molica,Monforte,Monforte,Zappala,Rizzo
, p. 269 - 274 (2007/10/03)
A series of 9-acetamido-1,2,3 4-tetrahydrocarbazoles (2) and 9-(aminoalkyloxyethyl)-1,2,3,4-tetrahydrocarbazoles (4) were prepared and tested for their in vitro antitumor activity. Compounds 4 are highly cytotoxic in almost all subpanel cell lines when te
