52867-93-3Relevant articles and documents
Synthesis and in silico evaluation of novel compounds for PET-based investigations of the norepinephrine transporter
Neudorfer, Catharina,Seddik, Amir,Shanab, Karem,Jurik, Andreas,Rami-Mark, Christina,Holzer, Wolfgang,Ecker, Gerhard,Mitterhauser, Markus,Wadsak, Wolfgang,Spreitzer, Helmut
, p. 1712 - 1730 (2015/01/30)
Since the norepinephrine transporter (NET) is involved in a variety of diseases, the investigation of underlying dysregulation-mechanisms of the norepinephrine (NE) system is of major interest. Based on the previously described highly potent and selective NET ligand 1-(3-(methylamino)-1-phenylpropyl)-3-phenyl-1,3-dihydro-2H-benzimidaz- ol-2-one (Me@APPI), this paper aims at the development of several fluorinated methylaminebased analogs of this compound. The newly synthesized compounds were computationally evaluated for their interactions with the monoamine transporters and represent reference compounds for PET-based investigation of the NET.
Imidazole analogues of fluoxetine, a novel class of anti-Candida agents
Silvestri, Romano,Artico, Marino,La Regina, Giuseppe,Di Pasquali, Alessandra,De Martino, Gabriella,D'Auria, Felicia Diodata,Nencioni, Lucia,Palamara, Anna Teresa
, p. 3924 - 3926 (2007/10/03)
Imidazole analogues of fluoxetine have been obtained by replacing the methylamino terminus of aminopropane chain with the imidazole ring. The newly designed imidazoles showed potent anti-Candida activity, superior to those of miconazole and other antifungal agents of clinical interest. 1-(4-Chlorophenyl)-l-(2,4-dichlorophenoxy)-3-(1H-imidazol-1-yl)propane (16), the most active among test imidazoles, Was about 2-fold more active and as much less cytotoxic than miconazole. High increase of activity was observed with methyl, nitro, fluorine, and chlorine (Cl > F > CH3 > NO2 > CF3).