13595-47-6Relevant academic research and scientific papers
A facile synthesis of 1-arenesulfonylazetidines through reaction of 1-arenesulfonylaziridines with dimethylsulfoxonium methylide generated under microwave irradiation
Malik, Sarika,Nadir, Upender K.
, p. 108 - 110 (2008/09/21)
A simple, efficient and general method has been developed for the synthesis of 1-arenesulfonylazetidines through a one-pot reaction of 1- arenesulfonylaziridines with dimethylsulfoxonium methylide, generated under microwave irradiation, using alumina as s
Novel acetylcholine and carbamoylcholine analogues: Development of a functionally selective α4β2 nicotinic acetylcholine receptor agonist
Hansen, Camilla P.,Jensen, Anders A.,Christensen, Jeppe K.,Balle, Thomas,Liljefors, Tommy,Fr?lund, Bente
scheme or table, p. 7380 - 7395 (2009/12/07)
A series of carbamoylcholine and acetylcholine analogues were synthesized and characterized pharmacologically at neuronal nicotinic acetylcholine receptors (nAChRs). Several of the compounds displayed low nanomolar binding affinities to the α4β2 nAChR and pronounced selectivity for this subtype over α3β4, α4β4, and α7 nAChRs. The high nAChR activity of carbamoylcholine analogue 5d was found to reside in its R-enantiomer, a characteristic most likely true for all other compounds in the series. Interestingly, the pronounced α4β2 selectivities exhibited by some of the compounds in the binding assays translated into functional selectivity. Compound 5a was a fairly potent partial α4β2 nAChR agonist with negligible activities at the α3β4 and α7 subtypes, thus being one of the few truly functionally selective α4β 2 nAChR agonists published to date. Ligand-protein docking experiments using homology models of the amino-terminal domains of α4β2 and α3β4 nAChRs identified residues Val111(β2)/Ile113(β4) , Phe119(β2)/Gln121(β4), and Thr155(α4)/Ser150(α3) as possible key determinants of the α4β2/α 3β4-selectivity displayed by the analogues.
Methylene Transfer from Dimethyloxosulphonium Methylide to N-Arylsulphonylaziridines: Stereospecific Synthesis of N-Arylsulphonylazetidines
Nadir, Upender K.,Sharma, Ms. Raman L.,Koul, Veerinder K.
, p. 2015 - 2020 (2007/10/02)
Several 2-alkyl, 2-aryl-, 2-benzyl-, 2,3-dialkyl- and 2,3-diarylsulphonylazetidines have been prepared in fair to good isolated yields through reaction of N-arylsulphonylaziridines with dimethyloxosulphonium methylide.Fused azetidines, however, could not
