3351-51-7Relevant academic research and scientific papers
Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors
Carocci, Alessia,Catalano, Alessia,Lovece, Angelo,Lentini, Giovanni,Duranti, Andrea,Lucini, Valeria,Pannacci, Marilou,Scaglione, Francesco,Franchini, Carlo
experimental part, p. 6496 - 6511 (2010/10/02)
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists.
Lead-discovery of bis-aromatic alkynes: A novel class of herbicides
Glock, Jutta,Allen, James,Niderman, Thierry,Haas, Hans Ulrich,Chollet, Renold,Eberle, Martin,Renold, Peter,Lutz, William,Ehrler, Juerg,Valentini, Marian,Walti, Markus,Sieger, Evelyne,Vettiger, Thomas,Brunner, Hans,Penzotti, Julie E.,Grootenhuis, Peter D. J.,Bondy, Steven,Comer, Daniel D.,Cheng, Soan,Steiger, Arthur,Zeller, Martin,Laue, Grit,Friedmann, Adrian,Jacob, Olivier,Nina, Mafalda,Widmer, Hans-Juerg,Kreuz, Klaus,Craig, G. Wayne
, p. 23 - 28 (2008/09/20)
The search for new active molecules with novel modes of action and desirable physical properties is an ongoing endeavour.[1,2] This publication describes the follow-up chemistry of a biological hit discovered in the screening system of Novartis
Electrochemically-induced spirolactonization of α-(methoxyphenoxy)alkanoic acids into quinone ketals
Deffieux, Denis,Fabre, Isabelle,Courseille, Christian,Quideau, Stephane
, p. 4458 - 4465 (2007/10/03)
Anodic oxidation of two series of α-(2)- and α-(4-methoxyphenoxy)alkanoic acids were studied both at the analytical and preparative scales in order to delineate mechanistic aspects of electrochemically induced spirolactonization and to develop synthetically useful orthoquinone bis- and monoketals. Although α-monomethylated carboxylic acids and acetic acid derivatives do not undergo any spiroannulation, α-dimethylated carboxylic acids furnished spirolactones in high yields. A gem-dimethyl effect is invoked to explain these differences in cyclization capacity. Electrooxidation conditions can be selected to furnish either quinone spirolactone bis- or monoketals. Chemoselective monohydrolysis of bisketals can also be accomplished in a stepwise fashion to furnish the corresponding spirolactone monoketals, but the ortho compound unfortunately dimerized in situ via a Diels-Alder process. An ECEC pathway is proposed to rationalize the observed spirolactonizations on the basis of cyclic voltammetry analyses.
