93138-61-5Relevant articles and documents
Indole, azaindole and related heterocyclic pyrrolidine derivatives
-
Page 26-27, (2008/06/13)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity
Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists
Itoh, Katsuhiko,Kanzaki, Koji,Ikebe, Tsuguo,Kuroita, Takanobu,Tomozane, Hideo,Sonda, Shuji,Sato, Noriko,Haga, Keiichiro,Kawakita, Takeshi
, p. 329 - 341 (2007/10/03)
A number of new carboxamide derivatives were synthesized. The affinity of these compounds for the serotoninergic 5-HT4 receptor was evaluated by use of radioligand-binding techniques. The agonistic activity was evaluated as the contractile effect of the ascending colon isolated from guinea-pigs. Among these compounds, 4-amino-5-chloro-2-methoxy-N-[l-[2- [(methylsulfonyl)amino]ethly]-4piperidinylmethyl]benzamide (24) showed a high affinity for the 5-HT4 receptor (Ki = 9.6 nM). Compound 24 displayed a higher affinity for 5-HT4 receptors than the other receptors, including, 5- HT3 and dopamine D2 receptors. In addition, compound 24 was confirmed to be a potent 5-HT4 receptor agonist (ED50 = 7.0 nM). An interaction model between compound 24 and 5-HT4 receptor was proposed.