15518-10-2Relevant articles and documents
Unforeseen Possibilities to Investigate the Regulation of Polyamine Metabolism Revealed by Novel C-Methylated Spermine Derivatives
Khomutov, Maxim,Hyv?nen, Mervi T.,Simonian, Alina,Formanovsky, Andrey A.,Mikhura, Irina V.,Chizhov, Alexander O.,Kochetkov, Sergey N.,Alhonen, Leena,Veps?l?inen, Jouko,Kein?nen, Tuomo A.,Khomutov, Alex R.
supporting information, p. 11335 - 11347 (2019/12/24)
The biogenic polyamines, spermine (Spm) and spermidine, are organic polycations present in millimolar concentrations in all eukaryotic cells participating in the regulation of vital cellular functions including proliferation and differentiation. The desig
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
experimental part, 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.
PROTECTION OF PRIMARY AND SECONDARY AMINES IN THE HYDROBORATION REACTION
Dicko, A.,Montury, M.,Baboulene, M.
, p. 6041 - 6044 (2007/10/02)
Trimethylsilyl groups are efficient to protect the N-H bonds of olefinic amines in the hydroboration reaction with BMS; deprotection is easily run with methanol and affords aminoorganoboranes which can be used without any oxydation.