671212-35-4Relevant academic research and scientific papers
Inhibition of Ebola virus infection: Identification of niemann-pick C1 as the target by optimization of a chemical probe
Lee, Kyungae,Ren, Tao,Co?té, Marceline,Gholamreza, Berahman,Misasi, John,Bruchez, Anna,Cunningham, James
supporting information, p. 239 - 243 (2013/03/28)
A high-throughput screen identified adamantane dipeptide 1 as an inhibitor of Ebola virus (EboV) infection. Hit-to-lead optimization to determine the structure-activity relationship (SAR) identified the more potent EboV inhibitor 2 and a photoaffinity labeling agent 3. These antiviral compounds were employed to identify the target as Niemann-Pick C1 (NPC1), a host protein that binds the EboV glycoprotein and is essential for infection. These studies establish NPC1 as a promising target for antiviral therapy.
From tyrosine to glycine: Synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor
Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cara, Carlota Lopez,Preti, Delia,Cruz-Lopez, Olga,Tabrizi, Mojgan Aghazadeh,Moorman, Allan R.,Gessi, Stefania,Fogli, Eleonora,Sacchetto, Valeria,Borea, Pier Andrea
, p. 3706 - 3715 (2008/02/09)
The characterization of the native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtype-selective antagonists with a "druglike" profile. However, a tyrosine derivative named KN-62 exhibits selective P2Xsub
Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
Scapecchi, Serena,Martini, Elisabetta,Manetti, Dina,Ghelardini, Carla,Martelli, Cecilia,Dei, Silvia,Galeotti, Nicoletta,Guandalini, Luca,Romanelli, Maria Novella,Teodori, Elisabetta
, p. 71 - 85 (2007/10/03)
Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
