76161-45-0Relevant academic research and scientific papers
Complete assignment of 1H and 13C NMR spectra of some α-arylthio and α-arylsulfonyl substituted N-methoxy-N-methyl propionamides
Domingues, Nelson L. C.,Mondino, Mirta G.,Reis, Adriana K. C. A.,Rittner, Roberto,Lima, Filipe S.,Olivato, Paulo R.
, p. 87 - 89 (2008/03/11)
The complete assignments of the 1H and 13C NMR spectra of the some α-arylthio and α-arylsulfonyl substituted N-methoxy-N-methyl propionamides, bearing methoxy, methyl, chloro, and nitro as substituents at the phenyl ring are reported
2-(4-R-Phenoxy/phenylthio)alkanoic esters of l-lupinine
Sparatore, Anna,Sparatore, Fabio
, p. 169 - 174 (2007/10/03)
Considering the great pharmacological interest in phenoxy/phenylthioalkanoic esters of open-chain or cyclic aminoalcohols, a set of ten such esters of lupinine was prepared. Initially, their ability to displace [3H]QNB from rat brain preparation was investigated. With the exception of two, all the prepared esters exhibited good affinity to muscarinic receptors (on a non-selective basis), with pKi in the range 6.67-7.68.
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters
Gualtieri,Bottalico,Calandrella,Dei,Giovannoni,Mealli,Romanelli,Scapecchi,Teodori,Galeotti,Ghelardini,Giotti,Bartolini
, p. 1712 - 1719 (2007/10/02)
Further modifications of the leads ((R)-(+)-hyoscyamine and (p- chlorophenyl)propionic acid α-tropanyl ester), which show analgesic and nootropic activities as a consequence of increased central presynaptic ACh release, are reported. 2-Phenoxy- and 2-(phenylthio)alkanoic acid esters showed the best results. Several members of these classes possess analgesic properties which are comparable to that of morphine and at the same time are able to reverse dicyclomine-induced amnesia. Confirmation was found that the mechanism of action is due to an increase in ACh release at central muscarinic synapses and that both auto- and heteroreceptors controlling ACh release are very likely involved. According to the results obtained with (R)- (+)-hyoscyamine, analgesic activity is stereochemistry dependent, since the R-(+)-enantiomers are always more efficacious than the corresponding S-(-)- ones. On the basis of their potency and acute toxicity, compounds (±)-28 (SM21) and (±)-42 (SM32) were selected for further study.
