37800-46-7Relevant academic research and scientific papers
Indole derivatives as dual-effective agents for the treatment of neurodegenerative diseases: Synthesis, biological evaluation, and molecular modeling studies
Buemi, Maria Rosa,De Luca, Laura,Chimirri, Alba,Ferro, Stefania,Gitto, Rosaria,Alvarez-Builla, Julio,Alajarin, Ramon
, p. 4575 - 4580 (2013/07/26)
Several indole derivatives, that were highly potent ligands of GluN2B-subunit-containing N-methyl-d-aspartate (NMDA) receptor, also demonstrated antioxidant properties in ABTS method. In particular, the 2-(4-benzylpiperidin-1-yl)-1-(5-hydroxy-1H-indol-3-yl)ethanone (1) proved to be a dual-effective neuroprotective agent. With the aim to increase the antioxidant properties we added a catechol moiety onto piperidine moiety. The designed hybrid derivative 3,4-dihydroxy-N-[1-[2-(5-hydroxy-1H-indol-3-yl)-2-oxoethyl] piperidin-4-yl]benzamide (10) was the most effective antioxidant agent (>94.1 ± 0.1% of inhibition at 17 μM) and showed GluN2B/NMDA receptor affinity at low micromolar concentration (IC50 0.66 μM). By means of computational studies we explored the effect of the presence of this antioxidant fragment during the recognition process to binding pocket.
SEPIAPTERIN REDUCTASE INHIBITORS FOR THE TREATMENT OF PAIN
-
Page/Page column 74, (2011/05/05)
Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and pro-drugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain)
Syntheses of β,β-difluorotryptamines
Deng, Wei-Ping,Nam, Ghilsoo,Fan, Junfa,Kirk, Kenneth L.
, p. 2798 - 2802 (2007/10/03)
Tryptamines disubstituted at the β-position with fluorine have been synthesized as part of our research program to study the effects of fluorine substitution on the biological activities of neuroactive amines. Treatment of N-Boc-3-azidoacetyl indoles, pre
Topsentin compounds effective against viruses and certain tumors
-
, (2008/06/13)
A new class of novel, biologically active bisindole alkaloid compounds, which have been named topsentins, pharmaceutical compositions containing them, methods of producing the compounds and methods of using them are disclosed. This new class of compounds
Topsentin, Bromotopsentin, and Dihydrodeoxybromotopsentin: Antiviral and Antitumor Bis(indolyl)imidazoles from Caribbean Deep-Sea Sponges of the Family Halichondriidae Structural and Synthetic Studies
Tsujii, Shinji,Rinehart, Kenneth L.,Gunasekera, Sarath P.,Kashman, Yoel,Cross, Susan S.,et al.
, p. 5446 - 5453 (2007/10/02)
Isolation and structure elucidation of topsentin (1) and bromotopsentin (2) are described.These novel indole alkaloids have been shown to have antitumor and antiviral activities.Their structures were determined on the basis of spectral data, and bromotopsentin was correlated structurally with topsentin by catalytic debromination.Syntheses of 1 and several analogues are also reported.
