GABA-uptake inhibitors: Construction of a general pharmacophore model and successful prediction of a new representative
A model for the pharmacophore of GABA-uptake inhibitors was established using published structure-activity data and molecular modeling. The model accounted for the activities of different classes of GABA-uptake inhibitors. Analogues of guvacine substituted at position 6 were synthesized in order to confirm the model. 6-(3,3-Diphenylpropyl)guvacine (30f), which fit well with the pharmacophore, had an in vitro IC50 of 0.1 μM. This value is as good as those of the best GABA-uptake inhibitors known today.
N'Goka,Schlewer,Linget,Chambon,Wermuth
p. 2547 - 2557
(2007/10/02)
Thiocarbonyl Olefination, IV. - Preparation of β-Amino Acids from N-(Acetyl)thioamides; Total Synthesis of Iturinic Acid
A new method for the synthesis of β-amino acids is described whose key step consists in the regioselective thiocarbonyl olefination of N-(acetyl)thioamides with methyl (triphenylphosphoranylidene)acetate.By this procedure, a straightforward synthesis of iturinic acid has been carried out for the first time.
Slopianka, Marion,Gossauer, Albert
p. 2258 - 2265
(2007/10/02)
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