1,720,963 research outputs found
Efficient Microwave and Phosphane-free Synthesis of Trisubstituted Olefins via Heck Coupling
No full textMicrowave assisted synthesis of chiral pyrrolines with biological activity
No full textA new, high yield regioselective reaction affording racemic and enantiomeric 1,2-dimethyl-3-[2-(6-substituted naphthyl)]-2H,5H-pyrrolines is reported. Compounds were provided by dehydration of the corresponding 1,2-dimethyl-3-[2-(6-substitutednaphthyl)]-3-hydroxypyrrolidines under microwave irradiation and solvent-free conditions. Pharmacological properties of enantiomeric compounds are also described; the analgesic activity was investigated by the hot plate test. A conformational analysis of the compounds was carried out by molecular modeling techniques with the aim to get information about the fitting to known analgesic pharmacophore models
Diastereoselective synthesis of chiral nonracemic naphthylaminoalcohols with analgesic activity
No full textAbstract—The diastereoselective synthesis of chiral nonracemic naphthylaminoalcohols has been accomplished. The diastereoisomers, obtained in high enantiomeric excesses, were investigated by 1H NMR and HPLC analyses. The configurational assignment was performed by NOESY 1H NMR spectroscopy. Pharmacological evaluation of the analgesic activity by means of the hot plate test is describe
Highly diastereoselective synthesis of enantiopure naphthylaminoalcohols with analgesic properties
No full textABSTRACT The diastereoselective synthesis via Grignard reaction of enantiopure
analgesic naphthylaminoalcohols has been performed. The chiral racemic key intermediate
3-dimethylamino-2-methyl-1-(naphthalen-2-yl)propan-1-one and enantiomers were
prepared and transformed into the desired compounds by addition of the organometallic
reagent. The chemical characterization of all diastereoisomers was accomplished by
1H NMR and HPLC analyses and the absolute configuration assigned by CD spectroscopy.
The in vitro and in vivo profile has also been evaluate
Risoluzione di ligandi selettivi sigma1 a struttura alchilamminoalchilarilica mediante HPLC chirale e studio configurazionale
No full textDerivati indolilalchilaminici. Approccio razionale alla progettazione di nuovi ligandi sigma
No full text
Chiral arylpyrrolidinols: preparation and biological profile
No full textAbstract—The preparation and biological evaluation of a new class of arylpyrrolidinols is reported. The antinociceptive activity was evaluated in vivo with the hot plate test (HPT) and formalin test (FT), excluding any involvement on motor coordination with the rota-rod test (RRT). The nociceptive behavior in the late phase of FT (representative of chronic pain) suggests an involvement of the antiinflammatory process and it is clearly influenced by the stereochemical features, being the eutomer of phenylpyrrolidinols, the (2R,3S) enantiomer. Despite this, a specific mechanism of action is not yet clarifie
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